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Selumetinib (AZD6244)
別名: ARRY-142886 中文名稱：司美替尼
Selumetinib (AZD6244, ARRY-142886)是一種有效，高選擇性的MEK抑制劑，對MEK1的IC50為14 nM，對MEK2的Kd值為530 nM。它也抑制ERK1/2磷酸化，IC50為10 nM，對p38α， MKK6， EGFR， ErbB2， ERK2， B-Raf等沒有抑制作用。Selumetinib可抑制細胞增殖、遷移并誘導凋亡。Phase 3。
Selumetinib (AZD6244) Chemical Structure
CAS: 606143-52-6
產品質控
批次：
純度：
99.80%
99.80
常與Selumetinib (AZD6244)一起在實驗中被使用的化合物
Selumetinib和Trametinib顯著抑制OMM2.5、OMM2.3和OMM1細胞的增殖。
Kassumeh S, et al. Int J Ophthalmol. 2022; 15(10): 1569–1576.
Selumetinib和Binimetinib對癌變細胞系iOvCa241(KRASG12D)和VOA-1312(KRASG12V)的增殖具有完全抑制作用。
Fernandez ML, et al. Am J Cancer Res. 2016 Oct 1;6(10):2235-2251. eCollection 2016.
Selumetinib和Cobimetinib是正在開發(fā)用于治療非小細胞肺癌的MEK抑制劑。
Kim C, et al. Expert Opin Investig Drugs. 2018 Jan;27(1):17-30.
Selumetinib和AZD0364聯(lián)合使用可導致多個KRAS突變異種移植模型中的腫瘤顯著消退。
Flemington V, et al. Mol Cancer Ther. 2021 Feb;20(2):238-249.
Selumetinib和AZD8055可增強KRAS突變人類NSCLC異種移植模型的抗腫瘤功效。
Selumetinib (AZD6244)相關產品
相關信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| A375 | Proliferation assay | 72 h | Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by Cell titer-glo assay, IC50=31 nM. | 23474388 | |
| SW480 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SW480 cells after 72 hrs by MTT assay, IC50 = 0.422 μM. | 27448918 | |
| SW620 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.015 μM. | 28038940 | |
| AsPC1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human AsPC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.0642 μM. | 28038940 | |
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.1 μM. | 28038940 | |
| SKCO1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SKCO1 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.117 μM. | 28038940 | |
| COLO205 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human COLO205 cells harboring BRAF mutant/wild type KRAS/wild type PIK3CA after 72 hrs by CCK8 assay, IC50 = 0.059 μM. | 29317148 | |
| HCC2998 | Growth inhibition assay | Inhibition of human HCC2998 cell growth in a cell viability assay, IC50 = 0.26907 μM. | SANGER | ||
| WM-115 | Growth inhibition assay | Inhibition of human WM-115 cell growth in a cell viability assay, IC50 = 0.26754 μM. | SANGER | ||
| RKO | Growth inhibition assay | Inhibition of human RKO cell growth in a cell viability assay, IC50 = 0.24838 μM. | SANGER | ||
| ONS-76 | Growth inhibition assay | Inhibition of human ONS-76 cell growth in a cell viability assay, IC50 = 0.24453 μM. | SANGER | ||
| A101D | Growth inhibition assay | Inhibition of human A101D cell growth in a cell viability assay, IC50 = 0.24033 μM. | SANGER | ||
| HTC-C3 | Growth inhibition assay | Inhibition of human HTC-C3 cell growth in a cell viability assay, IC50 = 0.21461 μM. | SANGER | ||
| A549 | Growth inhibition assay | Inhibition of human A549 cell growth in a cell viability assay, IC50 = 0.21413 μM. | SANGER | ||
| KU812 | Growth inhibition assay | Inhibition of human KU812 cell growth in a cell viability assay, IC50 = 0.21168 μM. | SANGER | ||
| HuP-T4 | Growth inhibition assay | Inhibition of human HuP-T4 cell growth in a cell viability assay, IC50 = 0.19532 μM. | SANGER | ||
| BPH-1 | Growth inhibition assay | Inhibition of human BPH-1 cell growth in a cell viability assay, IC50 = 0.18231 μM. | SANGER | ||
| SH-4 | Growth inhibition assay | Inhibition of human SH-4 cell growth in a cell viability assay, IC50 = 0.16648 μM. | SANGER | ||
| DOK | Growth inhibition assay | Inhibition of human DOK cell growth in a cell viability assay, IC50 = 0.14708 μM. | SANGER | ||
| EoL-1-cell | Growth inhibition assay | Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50 = 0.14476 μM. | SANGER | ||
| MEL-HO | Growth inhibition assay | Inhibition of human MEL-HO cell growth in a cell viability assay, IC50 = 0.13884 μM. | SANGER | ||
| CP50-MEL-B | Growth inhibition assay | Inhibition of human CP50-MEL-B cell growth in a cell viability assay, IC50 = 0.12794 μM. | SANGER | ||
| KY821 | Growth inhibition assay | Inhibition of human KY821 cell growth in a cell viability assay, IC50 = 0.10718 μM. | SANGER | ||
| BHT-101 | Growth inhibition assay | Inhibition of human BHT-101 cell growth in a cell viability assay, IC50 = 0.10693 μM. | SANGER | ||
| C32 | Growth inhibition assay | Inhibition of human C32 cell growth in a cell viability assay, IC50 = 0.09823 μM. | SANGER | ||
| LB2518-MEL | Growth inhibition assay | Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50 = 0.09382 μM. | SANGER | ||
| SK-N-AS | Growth inhibition assay | Inhibition of human SK-N-AS cell growth in a cell viability assay, IC50 = 0.09283 μM. | SANGER | ||
| HT-144 | Growth inhibition assay | Inhibition of human HT-144 cell growth in a cell viability assay, IC50 = 0.08905 μM. | SANGER | ||
| M14 | Growth inhibition assay | Inhibition of human M14 cell growth in a cell viability assay, IC50 = 0.03689 μM. | SANGER | ||
| DU-4475 | Growth inhibition assay | Inhibition of human DU-4475 cell growth in a cell viability assay, IC50 = 0.03367 μM. | SANGER | ||
| NOMO-1 | Growth inhibition assay | Inhibition of human NOMO-1 cell growth in a cell viability assay, IC50 = 0.03197 μM. | SANGER | ||
| HL-60 | Growth inhibition assay | Inhibition of human HL-60 cell growth in a cell viability assay, IC50 = 0.02459 μM. | SANGER | ||
| H9 | Growth inhibition assay | Inhibition of human H9 cell growth in a cell viability assay, IC50 = 0.02288 μM. | SANGER | ||
| CHP-212 | Growth inhibition assay | Inhibition of human CHP-212 cell growth in a cell viability assay, IC50 = 0.003153 μM. | SANGER | ||
| C2BBe1 | Growth inhibition assay | Inhibition of human C2BBe1 cell growth in a cell viability assay, IC50 = 0.27259 μM. | SANGER | ||
| RVH-421 | Growth inhibition assay | Inhibition of human RVH-421 cell growth in a cell viability assay, IC50 = 0.27939 μM. | SANGER | ||
| H-EMC-SS | Growth inhibition assay | Inhibition of human H-EMC-SS cell growth in a cell viability assay, IC50 = 0.29099 μM. | SANGER | ||
| ML-2 | Growth inhibition assay | Inhibition of human ML-2 cell growth in a cell viability assay, IC50 = 0.29363 μM. | SANGER | ||
| SW620 | Growth inhibition assay | Inhibition of human SW620 cell growth in a cell viability assay, IC50 = 0.3022 μM. | SANGER | ||
| UACC-257 | Growth inhibition assay | Inhibition of human UACC-257 cell growth in a cell viability assay, IC50 = 0.32184 μM. | SANGER | ||
| AsPC-1 | Growth inhibition assay | Inhibition of human AsPC-1 cell growth in a cell viability assay, IC50 = 0.32439 μM. | SANGER | ||
| CAL-39 | Growth inhibition assay | Inhibition of human CAL-39 cell growth in a cell viability assay, IC50 = 0.33226 μM. | SANGER | ||
| COLO-679 | Growth inhibition assay | Inhibition of human COLO-679 cell growth in a cell viability assay, IC50 = 0.34119 μM. | SANGER | ||
| NCI-H747 | Growth inhibition assay | Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50 = 0.35098 μM. | SANGER | ||
| NCI-H1437 | Growth inhibition assay | Inhibition of human NCI-H1437 cell growth in a cell viability assay, IC50 = 0.35285 μM. | SANGER | ||
| PSN1 | Growth inhibition assay | Inhibition of human PSN1 cell growth in a cell viability assay, IC50 = 0.36609 μM. | SANGER | ||
| NKM-1 | Growth inhibition assay | Inhibition of human NKM-1 cell growth in a cell viability assay, IC50 = 0.3858 μM. | SANGER | ||
| MZ2-MEL | Growth inhibition assay | Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50 = 0.39437 μM. | SANGER | ||
| SK-MEL-2 | Growth inhibition assay | Inhibition of human SK-MEL-2 cell growth in a cell viability assay, IC50 = 0.40506 μM. | SANGER | ||
| LAMA-84 | Growth inhibition assay | Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50 = 0.45622 μM. | SANGER | ||
| U-266 | Growth inhibition assay | Inhibition of human U-266 cell growth in a cell viability assay, IC50 = 0.48774 μM. | SANGER | ||
| RCM-1 | Growth inhibition assay | Inhibition of human RCM-1 cell growth in a cell viability assay, IC50 = 0.49385 μM. | SANGER | ||
| EM-2 | Growth inhibition assay | Inhibition of human EM-2 cell growth in a cell viability assay, IC50 = 0.51175 μM. | SANGER | ||
| Mewo | Growth inhibition assay | Inhibition of human Mewo cell growth in a cell viability assay, IC50 = 0.52101 μM. | SANGER | ||
| COLO-741 | Growth inhibition assay | Inhibition of human COLO-741 cell growth in a cell viability assay, IC50 = 0.53119 μM. | SANGER | ||
| ACN | Growth inhibition assay | Inhibition of human ACN cell growth in a cell viability assay, IC50 = 0.5669 μM. | SANGER | ||
| MV-4-11 | Growth inhibition assay | Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50 = 0.57543 μM. | SANGER | ||
| SW780 | Growth inhibition assay | Inhibition of human SW780 cell growth in a cell viability assay, IC50 = 0.66634 μM. | SANGER | ||
| JVM-3 | Growth inhibition assay | Inhibition of human JVM-3 cell growth in a cell viability assay, IC50 = 0.7006 μM. | SANGER | ||
| RPMI-8226 | Growth inhibition assay | Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50 = 0.74 μM. | SANGER | ||
| HO-1-N-1 | Growth inhibition assay | Inhibition of human HO-1-N-1 cell growth in a cell viability assay, IC50 = 0.74052 μM. | SANGER | ||
| BV-173 | Growth inhibition assay | Inhibition of human BV-173 cell growth in a cell viability assay, IC50 = 0.74802 μM. | SANGER | ||
| NCI-H2291 | Growth inhibition assay | Inhibition of human NCI-H2291 cell growth in a cell viability assay, IC50 = 0.76173 μM. | SANGER | ||
| SK-MEL-30 | Growth inhibition assay | Inhibition of human SK-MEL-30 cell growth in a cell viability assay, IC50 = 0.78171 μM. | SANGER | ||
| LB2241-RCC | Growth inhibition assay | Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50 = 0.78991 μM. | SANGER | ||
| LOXIMVI | Growth inhibition assay | Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50 = 0.85854 μM. | SANGER | ||
| HT-29 | Growth inhibition assay | Inhibition of human HT-29 cell growth in a cell viability assay, IC50 = 0.87319 μM. | SANGER | ||
| KG-1 | Growth inhibition assay | Inhibition of human KG-1 cell growth in a cell viability assay, IC50 = 0.89547 μM. | SANGER | ||
| SW954 | Growth inhibition assay | Inhibition of human SW954 cell growth in a cell viability assay, IC50 = 0.89645 μM. | SANGER | ||
| MIA-PaCa-2 | Growth inhibition assay | Inhibition of human MIA-PaCa-2 cell growth in a cell viability assay, IC50 = 0.89768 μM. | SANGER | ||
| HCE-T | Growth inhibition assay | Inhibition of human HCE-T cell growth in a cell viability assay, IC50 = 0.97131 μM. | SANGER | ||
| HN | Growth inhibition assay | Inhibition of human HN cell growth in a cell viability assay, IC50 = 1.00257 μM. | SANGER | ||
| LCLC-97TM1 | Growth inhibition assay | Inhibition of human LCLC-97TM1 cell growth in a cell viability assay, IC50 = 1.03191 μM. | SANGER | ||
| NB69 | Growth inhibition assay | Inhibition of human NB69 cell growth in a cell viability assay, IC50 = 1.0539 μM. | SANGER | ||
| LoVo | Growth inhibition assay | Inhibition of human LoVo cell growth in a cell viability assay, IC50 = 1.06231 μM. | SANGER | ||
| HCT-116 | Growth inhibition assay | Inhibition of human HCT-116 cell growth in a cell viability assay, IC50 = 1.06431 μM. | SANGER | ||
| AGS | Growth inhibition assay | Inhibition of human AGS cell growth in a cell viability assay, IC50 = 1.11831 μM. | SANGER | ||
| NCI-H292 | Growth inhibition assay | Inhibition of human NCI-H292 cell growth in a cell viability assay, IC50 = 1.1199 μM. | SANGER | ||
| P12-ICHIKAWA | Growth inhibition assay | Inhibition of human P12-ICHIKAWA cell growth in a cell viability assay, IC50 = 1.15899 μM. | SANGER | ||
| D-263MG | Growth inhibition assay | Inhibition of human D-263MG cell growth in a cell viability assay, IC50 = 1.18094 μM. | SANGER | ||
| COLO-792 | Growth inhibition assay | Inhibition of human COLO-792 cell growth in a cell viability assay, IC50 = 1.1863 μM. | SANGER | ||
| HSC-3 | Growth inhibition assay | Inhibition of human HSC-3 cell growth in a cell viability assay, IC50 = 1.18823 μM. | SANGER | ||
| NUGC-3 | Growth inhibition assay | Inhibition of human NUGC-3 cell growth in a cell viability assay, IC50 = 1.20379 μM. | SANGER | ||
| SW872 | Growth inhibition assay | Inhibition of human SW872 cell growth in a cell viability assay, IC50 = 1.26855 μM. | SANGER | ||
| HuCCT1 | Growth inhibition assay | Inhibition of human HuCCT1 cell growth in a cell viability assay, IC50 = 1.2996 μM. | SANGER | ||
| QIMR-WIL | Growth inhibition assay | Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50 = 1.34384 μM. | SANGER | ||
| NCI-H2087 | Growth inhibition assay | Inhibition of human NCI-H2087 cell growth in a cell viability assay, IC50 = 1.3751 μM. | SANGER | ||
| LS-513 | Growth inhibition assay | Inhibition of human LS-513 cell growth in a cell viability assay, IC50 = 1.42191 μM. | SANGER | ||
| CAL-54 | Growth inhibition assay | Inhibition of human CAL-54 cell growth in a cell viability assay, IC50 = 1.49314 μM. | SANGER | ||
| A204 | Growth inhibition assay | Inhibition of human A204 cell growth in a cell viability assay, IC50 = 1.51667 μM. | SANGER | ||
| CAL-62 | Growth inhibition assay | Inhibition of human CAL-62 cell growth in a cell viability assay, IC50 = 1.52292 μM. | SANGER | ||
| CAL-33 | Growth inhibition assay | Inhibition of human CAL-33 cell growth in a cell viability assay, IC50 = 1.54694 μM. | SANGER | ||
| COLO-678 | Growth inhibition assay | Inhibition of human COLO-678 cell growth in a cell viability assay, IC50 = 1.62382 μM. | SANGER | ||
| MEG-01 | Growth inhibition assay | Inhibition of human MEG-01 cell growth in a cell viability assay, IC50 = 1.62959 μM. | SANGER | ||
| HAL-01 | Growth inhibition assay | Inhibition of human HAL-01 cell growth in a cell viability assay, IC50 = 1.6957 μM. | SANGER | ||
| OAW-28 | Growth inhibition assay | Inhibition of human OAW-28 cell growth in a cell viability assay, IC50 = 1.74397 μM. | SANGER | ||
| NCI-SNU-1 | Growth inhibition assay | Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50 = 1.77243 μM. | SANGER | ||
| BHY | Growth inhibition assay | Inhibition of human BHY cell growth in a cell viability assay, IC50 = 1.81034 μM. | SANGER | ||
| EGI-1 | Growth inhibition assay | Inhibition of human EGI-1 cell growth in a cell viability assay, IC50 = 1.8282 μM. | SANGER | ||
| BB65-RCC | Growth inhibition assay | Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50 = 1.83855 μM. | SANGER | ||
| GAK | Growth inhibition assay | Inhibition of human GAK cell growth in a cell viability assay, IC50 = 1.90475 μM. | SANGER | ||
| SK-MEL-3 | Growth inhibition assay | Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50 = 1.95077 μM. | SANGER | ||
| KARPAS-45 | Growth inhibition assay | Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50 = 2.08248 μM. | SANGER | ||
| BCPAP | Growth inhibition assay | Inhibition of human BCPAP cell growth in a cell viability assay, IC50 = 2.1274 μM. | SANGER | ||
| RT-112 | Growth inhibition assay | Inhibition of human RT-112 cell growth in a cell viability assay, IC50 = 2.26046 μM. | SANGER | ||
| SK-HEP-1 | Growth inhibition assay | Inhibition of human SK-HEP-1 cell growth in a cell viability assay, IC50 = 2.29048 μM. | SANGER | ||
| Ca9-22 | Growth inhibition assay | Inhibition of human Ca9-22 cell growth in a cell viability assay, IC50 = 2.37667 μM. | SANGER | ||
| OS-RC-2 | Growth inhibition assay | Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50 = 2.40337 μM. | SANGER | ||
| BFTC-905 | Growth inhibition assay | Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50 = 2.42312 μM. | SANGER | ||
| HT-1080 | Growth inhibition assay | Inhibition of human HT-1080 cell growth in a cell viability assay, IC50 = 2.4301 μM. | SANGER | ||
| HCC2218 | Growth inhibition assay | Inhibition of human HCC2218 cell growth in a cell viability assay, IC50 = 2.48487 μM. | SANGER | ||
| KM12 | Growth inhibition assay | Inhibition of human KM12 cell growth in a cell viability assay, IC50 = 2.53961 μM. | SANGER | ||
| NB5 | Growth inhibition assay | Inhibition of human NB5 cell growth in a cell viability assay, IC50 = 2.56641 μM. | SANGER | ||
| BB30-HNC | Growth inhibition assay | Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50 = 2.71293 μM. | SANGER | ||
| NCI-H460 | Growth inhibition assay | Inhibition of human NCI-H460 cell growth in a cell viability assay, IC50 = 2.80274 μM. | SANGER | ||
| LAN-6 | Growth inhibition assay | Inhibition of human LAN-6 cell growth in a cell viability assay, IC50 = 2.82867 μM. | SANGER | ||
| EW-3 | Growth inhibition assay | Inhibition of human EW-3 cell growth in a cell viability assay, IC50 = 2.92505 μM. | SANGER | ||
| CAL-27 | Growth inhibition assay | Inhibition of human CAL-27 cell growth in a cell viability assay, IC50 = 3.06118 μM. | SANGER | ||
| COR-L105 | Growth inhibition assay | Inhibition of human COR-L105 cell growth in a cell viability assay, IC50 = 3.13462 μM. | SANGER | ||
| EFO-21 | Growth inhibition assay | Inhibition of human EFO-21 cell growth in a cell viability assay, IC50 = 3.19226 μM. | SANGER | ||
| MZ1-PC | Growth inhibition assay | Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50 = 3.31605 μM. | SANGER | ||
| EFO-27 | Growth inhibition assay | Inhibition of human EFO-27 cell growth in a cell viability assay, IC50 = 3.32612 μM. | SANGER | ||
| HPAF-II | Growth inhibition assay | Inhibition of human HPAF-II cell growth in a cell viability assay, IC50 = 3.33729 μM. | SANGER | ||
| KU-19-19 | Growth inhibition assay | Inhibition of human KU-19-19 cell growth in a cell viability assay, IC50 = 3.41951 μM. | SANGER | ||
| NCI-SNU-5 | Growth inhibition assay | Inhibition of human NCI-SNU-5 cell growth in a cell viability assay, IC50 = 3.61449 μM. | SANGER | ||
| LS-123 | Growth inhibition assay | Inhibition of human LS-123 cell growth in a cell viability assay, IC50 = 3.61831 μM. | SANGER | ||
| 769-P | Growth inhibition assay | Inhibition of human 769-P cell growth in a cell viability assay, IC50 = 3.7426 μM. | SANGER | ||
| SJSA-1 | Growth inhibition assay | Inhibition of human SJSA-1 cell growth in a cell viability assay, IC50 = 3.78146 μM. | SANGER | ||
| SK-LU-1 | Growth inhibition assay | Inhibition of human SK-LU-1 cell growth in a cell viability assay, IC50 = 3.86231 μM. | SANGER | ||
| A3-KAW | Growth inhibition assay | Inhibition of human A3-KAW cell growth in a cell viability assay, IC50 = 3.91055 μM. | SANGER | ||
| LB996-RCC | Growth inhibition assay | Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50 = 3.95043 μM. | SANGER | ||
| SN12C | Growth inhibition assay | Inhibition of human SN12C cell growth in a cell viability assay, IC50 = 3.95573 μM. | SANGER | ||
| COR-L23 | Growth inhibition assay | Inhibition of human COR-L23 cell growth in a cell viability assay, IC50 = 3.95669 μM. | SANGER | ||
| VM-CUB-1 | Growth inhibition assay | Inhibition of human VM-CUB-1 cell growth in a cell viability assay, IC50 = 3.96931 μM. | SANGER | ||
| RXF393 | Growth inhibition assay | Inhibition of human RXF393 cell growth in a cell viability assay, IC50 = 4.01591 μM. | SANGER | ||
| MOLT-13 | Growth inhibition assay | Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50 = 4.03419 μM. | SANGER | ||
| GCT | Growth inhibition assay | Inhibition of human GCT cell growth in a cell viability assay, IC50 = 4.10442 μM. | SANGER | ||
| SW1990 | Growth inhibition assay | Inhibition of human SW1990 cell growth in a cell viability assay, IC50 = 4.16622 μM. | SANGER | ||
| RD | Growth inhibition assay | Inhibition of human RD cell growth in a cell viability assay, IC50 = 4.19138 μM. | SANGER | ||
| HOP-92 | Growth inhibition assay | Inhibition of human HOP-92 cell growth in a cell viability assay, IC50 = 4.20093 μM. | SANGER | ||
| ME-180 | Growth inhibition assay | Inhibition of human ME-180 cell growth in a cell viability assay, IC50 = 4.25859 μM. | SANGER | ||
| MZ7-mel | Growth inhibition assay | Inhibition of human MZ7-mel cell growth in a cell viability assay, IC50 = 4.45265 μM. | SANGER | ||
| CAKI-1 | Growth inhibition assay | Inhibition of human CAKI-1 cell growth in a cell viability assay, IC50 = 4.46057 μM. | SANGER | ||
| YKG-1 | Growth inhibition assay | Inhibition of human YKG-1 cell growth in a cell viability assay, IC50 = 4.53421 μM. | SANGER | ||
| PANC-03-27 | Growth inhibition assay | Inhibition of human PANC-03-27 cell growth in a cell viability assay, IC50 = 4.53929 μM. | SANGER | ||
| A4-Fuk | Growth inhibition assay | Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50 = 4.54202 μM. | SANGER | ||
| NCI-H441 | Growth inhibition assay | Inhibition of human NCI-H441 cell growth in a cell viability assay, IC50 = 4.56342 μM. | SANGER | ||
| BxPC-3 | Growth inhibition assay | Inhibition of human BxPC-3 cell growth in a cell viability assay, IC50 = 4.65976 μM. | SANGER | ||
| ES3 | Growth inhibition assay | Inhibition of human ES3 cell growth in a cell viability assay, IC50 = 4.69173 μM. | SANGER | ||
| GP5d | Growth inhibition assay | Inhibition of human GP5d cell growth in a cell viability assay, IC50 = 4.78553 μM. | SANGER | ||
| CAL-85-1 | Growth inhibition assay | Inhibition of human CAL-85-1 cell growth in a cell viability assay, IC50 = 4.7942 μM. | SANGER | ||
| EPLC-272H | Growth inhibition assay | Inhibition of human EPLC-272H cell growth in a cell viability assay, IC50 = 4.81698 μM. | SANGER | ||
| HuP-T3 | Growth inhibition assay | Inhibition of human HuP-T3 cell growth in a cell viability assay, IC50 = 4.82408 μM. | SANGER | ||
| SW1710 | Growth inhibition assay | Inhibition of human SW1710 cell growth in a cell viability assay, IC50 = 5.03549 μM. | SANGER | ||
| TE-8 | Growth inhibition assay | Inhibition of human TE-8 cell growth in a cell viability assay, IC50 = 5.06911 μM. | SANGER | ||
| TE-12 | Growth inhibition assay | Inhibition of human TE-12 cell growth in a cell viability assay, IC50 = 5.13703 μM. | SANGER | ||
| NCI-H1573 | Growth inhibition assay | Inhibition of human NCI-H1573 cell growth in a cell viability assay, IC50 = 5.27238 μM. | SANGER | ||
| SW1417 | Growth inhibition assay | Inhibition of human SW1417 cell growth in a cell viability assay, IC50 = 5.27398 μM. | SANGER | ||
| CHL-1 | Growth inhibition assay | Inhibition of human CHL-1 cell growth in a cell viability assay, IC50 = 5.3199 μM. | SANGER | ||
| Calu-6 | Growth inhibition assay | Inhibition of human Calu-6 cell growth in a cell viability assay, IC50 = 5.42927 μM. | SANGER | ||
| MDA-MB-231 | Growth inhibition assay | Inhibition of human MDA-MB-231 cell growth in a cell viability assay, IC50 = 5.56523 μM. | SANGER | ||
| SCC-25 | Growth inhibition assay | Inhibition of human SCC-25 cell growth in a cell viability assay, IC50 = 5.97121 μM. | SANGER | ||
| 639-V | Growth inhibition assay | Inhibition of human 639-V cell growth in a cell viability assay, IC50 = 6.12933 μM. | SANGER | ||
| D-502MG | Growth inhibition assay | Inhibition of human D-502MG cell growth in a cell viability assay, IC50 = 6.17659 μM. | SANGER | ||
| PANC-10-05 | Growth inhibition assay | Inhibition of human PANC-10-05 cell growth in a cell viability assay, IC50 = 6.20181 μM. | SANGER | ||
| Ramos-2G6-4C10 | Growth inhibition assay | Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50 = 6.27094 μM. | SANGER | ||
| NB10 | Growth inhibition assay | Inhibition of human NB10 cell growth in a cell viability assay, IC50 = 6.32533 μM. | SANGER | ||
| MSTO-211H | Growth inhibition assay | Inhibition of human MSTO-211H cell growth in a cell viability assay, IC50 = 6.4008 μM. | SANGER | ||
| NCI-H1651 | Growth inhibition assay | Inhibition of human NCI-H1651 cell growth in a cell viability assay, IC50 = 6.65328 μM. | SANGER | ||
| 697 | Growth inhibition assay | Inhibition of human 697 cell growth in a cell viability assay, IC50 = 6.67397 μM. | SANGER | ||
| HCC70 | Growth inhibition assay | Inhibition of human HCC70 cell growth in a cell viability assay, IC50 = 6.68865 μM. | SANGER | ||
| SW1116 | Growth inhibition assay | Inhibition of human SW1116 cell growth in a cell viability assay, IC50 = 6.81297 μM. | SANGER | ||
| SK-MES-1 | Growth inhibition assay | Inhibition of human SK-MES-1 cell growth in a cell viability assay, IC50 = 6.8488 μM. | SANGER | ||
| GCIY | Growth inhibition assay | Inhibition of human GCIY cell growth in a cell viability assay, IC50 = 6.91962 μM. | SANGER | ||
| GMS-10 | Growth inhibition assay | Inhibition of human GMS-10 cell growth in a cell viability assay, IC50 = 7.07755 μM. | SANGER | ||
| NCI-H1092 | Growth inhibition assay | Inhibition of human NCI-H1092 cell growth in a cell viability assay, IC50 = 7.15334 μM. | SANGER | ||
| CFPAC-1 | Growth inhibition assay | Inhibition of human CFPAC-1 cell growth in a cell viability assay, IC50 = 7.22101 μM. | SANGER | ||
| TK10 | Growth inhibition assay | Inhibition of human TK10 cell growth in a cell viability assay, IC50 = 7.35587 μM. | SANGER | ||
| FADU | Growth inhibition assay | Inhibition of human FADU cell growth in a cell viability assay, IC50 = 7.5093 μM. | SANGER | ||
| 8305C | Growth inhibition assay | Inhibition of human 8305C cell growth in a cell viability assay, IC50 = 7.85355 μM. | SANGER | ||
| DK-MG | Growth inhibition assay | Inhibition of human DK-MG cell growth in a cell viability assay, IC50 = 7.94937 μM. | SANGER | ||
| BFTC-909 | Growth inhibition assay | Inhibition of human BFTC-909 cell growth in a cell viability assay, IC50 = 7.97836 μM. | SANGER | ||
| IGR-1 | Growth inhibition assay | Inhibition of human IGR-1 cell growth in a cell viability assay, IC50 = 8.18051 μM. | SANGER | ||
| MDA-MB-361 | Growth inhibition assay | Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50 = 8.1824 μM. | SANGER | ||
| KYSE-150 | Growth inhibition assay | Inhibition of human KYSE-150 cell growth in a cell viability assay, IC50 = 8.21937 μM. | SANGER | ||
| DB | Growth inhibition assay | Inhibition of human DB cell growth in a cell viability assay, IC50 = 8.36905 μM. | SANGER | ||
| NH-12 | Growth inhibition assay | Inhibition of human NH-12 cell growth in a cell viability assay, IC50 = 8.42736 μM. | SANGER | ||
| CTV-1 | Growth inhibition assay | Inhibition of human CTV-1 cell growth in a cell viability assay, IC50 = 8.43337 μM. | SANGER | ||
| A498 | Growth inhibition assay | Inhibition of human A498 cell growth in a cell viability assay, IC50 = 8.78475 μM. | SANGER | ||
| LS-1034 | Growth inhibition assay | Inhibition of human LS-1034 cell growth in a cell viability assay, IC50 = 8.96464 μM. | SANGER | ||
| FTC-133 | Growth inhibition assay | Inhibition of human FTC-133 cell growth in a cell viability assay, IC50 = 8.98459 μM. | SANGER | ||
| TGBC11TKB | Growth inhibition assay | Inhibition of human TGBC11TKB cell growth in a cell viability assay, IC50 = 9.10836 μM. | SANGER | ||
| SK-MEL-1 | Growth inhibition assay | Inhibition of human SK-MEL-1 cell growth in a cell viability assay, IC50 = 9.19136 μM. | SANGER | ||
| RPMI-7951 | Growth inhibition assay | Inhibition of human RPMI-7951 cell growth in a cell viability assay, IC50 = 9.25201 μM. | SANGER | ||
| GT3TKB | Growth inhibition assay | Inhibition of human GT3TKB cell growth in a cell viability assay, IC50 = 9.37403 μM. | SANGER | ||
| SW962 | Growth inhibition assay | Inhibition of human SW962 cell growth in a cell viability assay, IC50 = 9.52325 μM. | SANGER | ||
| T-24 | Growth inhibition assay | Inhibition of human T-24 cell growth in a cell viability assay, IC50 = 9.65807 μM. | SANGER | ||
| DBTRG-05MG | Growth inhibition assay | Inhibition of human DBTRG-05MG cell growth in a cell viability assay, IC50 = 9.75666 μM. | SANGER | ||
| G-401 | Growth inhibition assay | Inhibition of human G-401 cell growth in a cell viability assay, IC50 = 10.0739 μM. | SANGER | ||
| RS4-11 | Growth inhibition assay | Inhibition of human RS4-11 cell growth in a cell viability assay, IC50 = 10.2791 μM. | SANGER | ||
| KGN | Growth inhibition assay | Inhibition of human KGN cell growth in a cell viability assay, IC50 = 10.4046 μM. | SANGER | ||
| 786-0 | Growth inhibition assay | Inhibition of human 786-0 cell growth in a cell viability assay, IC50 = 10.4166 μM. | SANGER | ||
| EW-18 | Growth inhibition assay | Inhibition of human EW-18 cell growth in a cell viability assay, IC50 = 10.4366 μM. | SANGER | ||
| DEL | Growth inhibition assay | Inhibition of human DEL cell growth in a cell viability assay, IC50 = 10.545 μM. | SANGER | ||
| HuH-7 | Growth inhibition assay | Inhibition of human HuH-7 cell growth in a cell viability assay, IC50 = 10.5705 μM. | SANGER | ||
| MG-63 | Growth inhibition assay | Inhibition of human MG-63 cell growth in a cell viability assay, IC50 = 10.7333 μM. | SANGER | ||
| A253 | Growth inhibition assay | Inhibition of human A253 cell growth in a cell viability assay, IC50 = 10.7902 μM. | SANGER | ||
| TGW | Growth inhibition assay | Inhibition of human TGW cell growth in a cell viability assay, IC50 = 10.7937 μM. | SANGER | ||
| HH | Growth inhibition assay | Inhibition of human HH cell growth in a cell viability assay, IC50 = 10.8062 μM. | SANGER | ||
| LS-411N | Growth inhibition assay | Inhibition of human LS-411N cell growth in a cell viability assay, IC50 = 10.8244 μM. | SANGER | ||
| NCI-H2347 | Growth inhibition assay | Inhibition of human NCI-H2347 cell growth in a cell viability assay, IC50 = 10.8437 μM. | SANGER | ||
| LU-65 | Growth inhibition assay | Inhibition of human LU-65 cell growth in a cell viability assay, IC50 = 10.9226 μM. | SANGER | ||
| TE-11 | Growth inhibition assay | Inhibition of human TE-11 cell growth in a cell viability assay, IC50 = 11.025 μM. | SANGER | ||
| SBC-1 | Growth inhibition assay | Inhibition of human SBC-1 cell growth in a cell viability assay, IC50 = 11.1032 μM. | SANGER | ||
| TGBC24TKB | Growth inhibition assay | Inhibition of human TGBC24TKB cell growth in a cell viability assay, IC50 = 11.118 μM. | SANGER | ||
| ECC10 | Growth inhibition assay | Inhibition of human ECC10 cell growth in a cell viability assay, IC50 = 11.2283 μM. | SANGER | ||
| GR-ST | Growth inhibition assay | Inhibition of human GR-ST cell growth in a cell viability assay, IC50 = 11.268 μM. | SANGER | ||
| NCI-H720 | Growth inhibition assay | Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50 = 11.3977 μM. | SANGER | ||
| VA-ES-BJ | Growth inhibition assay | Inhibition of human VA-ES-BJ cell growth in a cell viability assay, IC50 = 11.5513 μM. | SANGER | ||
| MOLT-16 | Growth inhibition assay | Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50 = 12.1161 μM. | SANGER | ||
| KYSE-140 | Growth inhibition assay | Inhibition of human KYSE-140 cell growth in a cell viability assay, IC50 = 12.1596 μM. | SANGER | ||
| SCC-4 | Growth inhibition assay | Inhibition of human SCC-4 cell growth in a cell viability assay, IC50 = 12.24 μM. | SANGER | ||
| NCI-H1155 | Growth inhibition assay | Inhibition of human NCI-H1155 cell growth in a cell viability assay, IC50 = 12.3017 μM. | SANGER | ||
| OCUB-M | Growth inhibition assay | Inhibition of human OCUB-M cell growth in a cell viability assay, IC50 = 12.3189 μM. | SANGER | ||
| MN-60 | Growth inhibition assay | Inhibition of human MN-60 cell growth in a cell viability assay, IC50 = 12.3732 μM. | SANGER | ||
| RO82-W-1 | Growth inhibition assay | Inhibition of human RO82-W-1 cell growth in a cell viability assay, IC50 = 12.3879 μM. | SANGER | ||
| KOSC-2 | Growth inhibition assay | Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50 = 12.5508 μM. | SANGER | ||
| L-363 | Growth inhibition assay | Inhibition of human L-363 cell growth in a cell viability assay, IC50 = 12.5925 μM. | SANGER | ||
| NCI-H661 | Growth inhibition assay | Inhibition of human NCI-H661 cell growth in a cell viability assay, IC50 = 12.8587 μM. | SANGER | ||
| KYSE-450 | Growth inhibition assay | Inhibition of human KYSE-450 cell growth in a cell viability assay, IC50 = 13.0396 μM. | SANGER | ||
| TI-73 | Growth inhibition assay | Inhibition of human TI-73 cell growth in a cell viability assay, IC50 = 13.044 μM. | SANGER | ||
| KNS-81-FD | Growth inhibition assay | Inhibition of human KNS-81-FD cell growth in a cell viability assay, IC50 = 13.0748 μM. | SANGER | ||
| HCC1954 | Growth inhibition assay | Inhibition of human HCC1954 cell growth in a cell viability assay, IC50 = 13.2783 μM. | SANGER | ||
| A427 | Growth inhibition assay | Inhibition of human A427 cell growth in a cell viability assay, IC50 = 13.6689 μM. | SANGER | ||
| MOLT-4 | Growth inhibition assay | Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50 = 13.8531 μM. | SANGER | ||
| U-118-MG | Growth inhibition assay | Inhibition of human U-118-MG cell growth in a cell viability assay, IC50 = 13.8702 μM. | SANGER | ||
| SF126 | Growth inhibition assay | Inhibition of human SF126 cell growth in a cell viability assay, IC50 = 13.9165 μM. | SANGER | ||
| SF539 | Growth inhibition assay | Inhibition of human SF539 cell growth in a cell viability assay, IC50 = 13.9474 μM. | SANGER | ||
| Daoy | Growth inhibition assay | Inhibition of human Daoy cell growth in a cell viability assay, IC50 = 14.4979 μM. | SANGER | ||
| DoTc2-4510 | Growth inhibition assay | Inhibition of human DoTc2-4510 cell growth in a cell viability assay, IC50 = 14.5175 μM. | SANGER | ||
| TYK-nu | Growth inhibition assay | Inhibition of human TYK-nu cell growth in a cell viability assay, IC50 = 14.56 μM. | SANGER | ||
| CGTH-W-1 | Growth inhibition assay | Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50 = 14.8483 μM. | SANGER | ||
| HuO9 | Growth inhibition assay | Inhibition of human HuO9 cell growth in a cell viability assay, IC50 = 15.063 μM. | SANGER | ||
| EW-16 | Growth inhibition assay | Inhibition of human EW-16 cell growth in a cell viability assay, IC50 = 15.0949 μM. | SANGER | ||
| NCI-H630 | Growth inhibition assay | Inhibition of human NCI-H630 cell growth in a cell viability assay, IC50 = 15.1613 μM. | SANGER | ||
| CAL-12T | Growth inhibition assay | Inhibition of human CAL-12T cell growth in a cell viability assay, IC50 = 15.331 μM. | SANGER | ||
| TE-5 | Growth inhibition assay | Inhibition of human TE-5 cell growth in a cell viability assay, IC50 = 15.6133 μM. | SANGER | ||
| U251 | Growth inhibition assay | Inhibition of human U251 cell growth in a cell viability assay, IC50 = 15.7383 μM. | SANGER | ||
| BB49-HNC | Growth inhibition assay | Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50 = 16.506 μM. | SANGER | ||
| OCI-AML2 | Growth inhibition assay | Inhibition of human OCI-AML2 cell growth in a cell viability assay, IC50 = 16.665 μM. | SANGER | ||
| KINGS-1 | Growth inhibition assay | Inhibition of human KINGS-1 cell growth in a cell viability assay, IC50 = 16.6918 μM. | SANGER | ||
| D-566MG | Growth inhibition assay | Inhibition of human D-566MG cell growth in a cell viability assay, IC50 = 16.7262 μM. | SANGER | ||
| P30-OHK | Growth inhibition assay | Inhibition of human P30-OHK cell growth in a cell viability assay, IC50 = 16.9068 μM. | SANGER | ||
| GAMG | Growth inhibition assay | Inhibition of human GAMG cell growth in a cell viability assay, IC50 = 16.9243 μM. | SANGER | ||
| HCC1419 | Growth inhibition assay | Inhibition of human HCC1419 cell growth in a cell viability assay, IC50 = 17.6139 μM. | SANGER | ||
| SNU-C2B | Growth inhibition assay | Inhibition of human SNU-C2B cell growth in a cell viability assay, IC50 = 17.7377 μM. | SANGER | ||
| MHH-NB-11 | Growth inhibition assay | Inhibition of human MHH-NB-11 cell growth in a cell viability assay, IC50 = 18.1383 μM. | SANGER | ||
| COLO-684 | Growth inhibition assay | Inhibition of human COLO-684 cell growth in a cell viability assay, IC50 = 18.2383 μM. | SANGER | ||
| OC-314 | Growth inhibition assay | Inhibition of human OC-314 cell growth in a cell viability assay, IC50 = 18.358 μM. | SANGER | ||
| Becker | Growth inhibition assay | Inhibition of human Becker cell growth in a cell viability assay, IC50 = 18.4623 μM. | SANGER | ||
| NCI-H1623 | Growth inhibition assay | Inhibition of human NCI-H1623 cell growth in a cell viability assay, IC50 = 18.6368 μM. | SANGER | ||
| IGROV-1 | Growth inhibition assay | Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50 = 18.6559 μM. | SANGER | ||
| HSC-2 | Growth inhibition assay | Inhibition of human HSC-2 cell growth in a cell viability assay, IC50 = 18.9577 μM. | SANGER | ||
| RMG-I | Growth inhibition assay | Inhibition of human RMG-I cell growth in a cell viability assay, IC50 = 19.1338 μM. | SANGER | ||
| CAL-120 | Growth inhibition assay | Inhibition of human CAL-120 cell growth in a cell viability assay, IC50 = 19.2354 μM. | SANGER | ||
| GB-1 | Growth inhibition assay | Inhibition of human GB-1 cell growth in a cell viability assay, IC50 = 19.7444 μM. | SANGER | ||
| LU-139 | Growth inhibition assay | Inhibition of human LU-139 cell growth in a cell viability assay, IC50 = 20.1816 μM. | SANGER | ||
| HT-1376 | Growth inhibition assay | Inhibition of human HT-1376 cell growth in a cell viability assay, IC50 = 20.5772 μM. | SANGER | ||
| SW982 | Growth inhibition assay | Inhibition of human SW982 cell growth in a cell viability assay, IC50 = 20.6837 μM. | SANGER | ||
| SK-N-FI | Growth inhibition assay | Inhibition of human SK-N-FI cell growth in a cell viability assay, IC50 = 21.0886 μM. | SANGER | ||
| SCC-9 | Growth inhibition assay | Inhibition of human SCC-9 cell growth in a cell viability assay, IC50 = 21.1409 μM. | SANGER | ||
| SW756 | Growth inhibition assay | Inhibition of human SW756 cell growth in a cell viability assay, IC50 = 21.2156 μM. | SANGER | ||
| SW948 | Growth inhibition assay | Inhibition of human SW948 cell growth in a cell viability assay, IC50 = 21.5236 μM. | SANGER | ||
| SW1573 | Growth inhibition assay | Inhibition of human SW1573 cell growth in a cell viability assay, IC50 = 21.8345 μM. | SANGER | ||
| NCI-H1792 | Growth inhibition assay | Inhibition of human NCI-H1792 cell growth in a cell viability assay, IC50 = 21.8565 μM. | SANGER | ||
| BE-13 | Growth inhibition assay | Inhibition of human BE-13 cell growth in a cell viability assay, IC50 = 22.5873 μM. | SANGER | ||
| SK-OV-3 | Growth inhibition assay | Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50 = 22.7388 μM. | SANGER | ||
| PA-1 | Growth inhibition assay | Inhibition of human PA-1 cell growth in a cell viability assay, IC50 = 22.8712 μM. | SANGER | ||
| NCI-H1693 | Growth inhibition assay | Inhibition of human NCI-H1693 cell growth in a cell viability assay, IC50 = 22.9313 μM. | SANGER | ||
| no-10 | Growth inhibition assay | Inhibition of human no-10 cell growth in a cell viability assay, IC50 = 23.3588 μM. | SANGER | ||
| JVM-2 | Growth inhibition assay | Inhibition of human JVM-2 cell growth in a cell viability assay, IC50 = 23.4147 μM. | SANGER | ||
| SK-NEP-1 | Growth inhibition assay | Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50 = 23.5205 μM. | SANGER | ||
| PC-3 | Growth inhibition assay | Inhibition of human PC-3 cell growth in a cell viability assay, IC50 = 23.5722 μM. | SANGER | ||
| U-2-OS | Growth inhibition assay | Inhibition of human U-2-OS cell growth in a cell viability assay, IC50 = 23.8469 μM. | SANGER | ||
| NBsusSR | Growth inhibition assay | Inhibition of human NBsusSR cell growth in a cell viability assay, IC50 = 24.1062 μM. | SANGER | ||
| EW-13 | Growth inhibition assay | Inhibition of human EW-13 cell growth in a cell viability assay, IC50 = 24.1398 μM. | SANGER | ||
| BT-20 | Growth inhibition assay | Inhibition of human BT-20 cell growth in a cell viability assay, IC50 = 24.7178 μM. | SANGER | ||
| MS-1 | Growth inhibition assay | Inhibition of human MS-1 cell growth in a cell viability assay, IC50 = 25.0498 μM. | SANGER | ||
| HCC1187 | Growth inhibition assay | Inhibition of human HCC1187 cell growth in a cell viability assay, IC50 = 25.4451 μM. | SANGER | ||
| TE-1 | Growth inhibition assay | Inhibition of human TE-1 cell growth in a cell viability assay, IC50 = 25.6953 μM. | SANGER | ||
| MKN7 | Growth inhibition assay | Inhibition of human MKN7 cell growth in a cell viability assay, IC50 = 25.7913 μM. | SANGER | ||
| NCI-H727 | Growth inhibition assay | Inhibition of human NCI-H727 cell growth in a cell viability assay, IC50 = 26.0513 μM. | SANGER | ||
| H4 | Growth inhibition assay | Inhibition of human H4 cell growth in a cell viability assay, IC50 = 26.3768 μM. | SANGER | ||
| 647-V | Growth inhibition assay | Inhibition of human 647-V cell growth in a cell viability assay, IC50 = 26.8811 μM. | SANGER | ||
| KM-H2 | Growth inhibition assay | Inhibition of human KM-H2 cell growth in a cell viability assay, IC50 = 26.924 μM. | SANGER | ||
| ABC-1 | Growth inhibition assay | Inhibition of human ABC-1 cell growth in a cell viability assay, IC50 = 27.1974 μM. | SANGER | ||
| HCC1806 | Growth inhibition assay | Inhibition of human HCC1806 cell growth in a cell viability assay, IC50 = 27.3422 μM. | SANGER | ||
| ES5 | Growth inhibition assay | Inhibition of human ES5 cell growth in a cell viability assay, IC50 = 27.4999 μM. | SANGER | ||
| C3A | Growth inhibition assay | Inhibition of human C3A cell growth in a cell viability assay, IC50 = 27.5694 μM. | SANGER | ||
| TE-10 | Growth inhibition assay | Inhibition of human TE-10 cell growth in a cell viability assay, IC50 = 27.6356 μM. | SANGER | ||
| S-117 | Growth inhibition assay | Inhibition of human S-117 cell growth in a cell viability assay, IC50 = 27.7571 μM. | SANGER | ||
| TGBC1TKB | Growth inhibition assay | Inhibition of human TGBC1TKB cell growth in a cell viability assay, IC50 = 27.9902 μM. | SANGER | ||
| NCI-H1793 | Growth inhibition assay | Inhibition of human NCI-H1793 cell growth in a cell viability assay, IC50 = 28.3076 μM. | SANGER | ||
| ES4 | Growth inhibition assay | Inhibition of human ES4 cell growth in a cell viability assay, IC50 = 28.7352 μM. | SANGER | ||
| AN3-CA | Growth inhibition assay | Inhibition of human AN3-CA cell growth in a cell viability assay, IC50 = 28.8593 μM. | SANGER | ||
| NMC-G1 | Growth inhibition assay | Inhibition of human NMC-G1 cell growth in a cell viability assay, IC50 = 29.111 μM. | SANGER | ||
| NCI-H226 | Growth inhibition assay | Inhibition of human NCI-H226 cell growth in a cell viability assay, IC50 = 29.2701 μM. | SANGER | ||
| NCI-H522 | Growth inhibition assay | Inhibition of human NCI-H522 cell growth in a cell viability assay, IC50 = 29.8339 μM. | SANGER | ||
| SW48 | Growth inhibition assay | Inhibition of human SW48 cell growth in a cell viability assay, IC50 = 29.9252 μM. | SANGER | ||
| OE33 | Growth inhibition assay | Inhibition of human OE33 cell growth in a cell viability assay, IC50 = 30.7954 μM. | SANGER | ||
| NCI-H2228 | Growth inhibition assay | Inhibition of human NCI-H2228 cell growth in a cell viability assay, IC50 = 31.0344 μM. | SANGER | ||
| D-423MG | Growth inhibition assay | Inhibition of human D-423MG cell growth in a cell viability assay, IC50 = 31.0564 μM. | SANGER | ||
| IST-MEL1 | Growth inhibition assay | Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50 = 31.1528 μM. | SANGER | ||
| A388 | Growth inhibition assay | Inhibition of human A388 cell growth in a cell viability assay, IC50 = 31.6236 μM. | SANGER | ||
| LN-405 | Growth inhibition assay | Inhibition of human LN-405 cell growth in a cell viability assay, IC50 = 31.7983 μM. | SANGER | ||
| DMS-273 | Growth inhibition assay | Inhibition of human DMS-273 cell growth in a cell viability assay, IC50 = 31.9138 μM. | SANGER | ||
| KS-1 | Growth inhibition assay | Inhibition of human KS-1 cell growth in a cell viability assay, IC50 = 33.1321 μM. | SANGER | ||
| NCI-H209 | Growth inhibition assay | Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50 = 33.4517 μM. | SANGER | ||
| HOS | Growth inhibition assay | Inhibition of human HOS cell growth in a cell viability assay, IC50 = 33.7253 μM. | SANGER | ||
| GI-1 | Growth inhibition assay | Inhibition of human GI-1 cell growth in a cell viability assay, IC50 = 33.8071 μM. | SANGER | ||
| RERF-LC-MS | Growth inhibition assay | Inhibition of human RERF-LC-MS cell growth in a cell viability assay, IC50 = 34.0315 μM. | SANGER | ||
| NCI-H526 | Growth inhibition assay | Inhibition of human NCI-H526 cell growth in a cell viability assay, IC50 = 34.076 μM. | SANGER | ||
| RPMI-2650 | Growth inhibition assay | Inhibition of human RPMI-2650 cell growth in a cell viability assay, IC50 = 34.4334 μM. | SANGER | ||
| KYSE-70 | Growth inhibition assay | Inhibition of human KYSE-70 cell growth in a cell viability assay, IC50 = 34.8426 μM. | SANGER | ||
| Capan-2 | Growth inhibition assay | Inhibition of human Capan-2 cell growth in a cell viability assay, IC50 = 36.4652 μM. | SANGER | ||
| OVCAR-4 | Growth inhibition assay | Inhibition of human OVCAR-4 cell growth in a cell viability assay, IC50 = 37.2176 μM. | SANGER | ||
| OVCAR-8 | Growth inhibition assay | Inhibition of human OVCAR-8 cell growth in a cell viability assay, IC50 = 37.9823 μM. | SANGER | ||
| NCI-H1355 | Growth inhibition assay | Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50 = 38.1051 μM. | SANGER | ||
| COLO-680N | Growth inhibition assay | Inhibition of human COLO-680N cell growth in a cell viability assay, IC50 = 38.2429 μM. | SANGER | ||
| NCI-H2122 | Growth inhibition assay | Inhibition of human NCI-H2122 cell growth in a cell viability assay, IC50 = 39.3363 μM. | SANGER | ||
| Saos-2 | Growth inhibition assay | Inhibition of human Saos-2 cell growth in a cell viability assay, IC50 = 39.7053 μM. | SANGER | ||
| HCC2157 | Growth inhibition assay | Inhibition of human HCC2157 cell growth in a cell viability assay, IC50 = 40.7734 μM. | SANGER | ||
| VMRC-RCZ | Growth inhibition assay | Inhibition of human VMRC-RCZ cell growth in a cell viability assay, IC50 = 41.2962 μM. | SANGER | ||
| ETK-1 | Growth inhibition assay | Inhibition of human ETK-1 cell growth in a cell viability assay, IC50 = 41.5751 μM. | SANGER | ||
| RCC10RGB | Growth inhibition assay | Inhibition of human RCC10RGB cell growth in a cell viability assay, IC50 = 42.018 μM. | SANGER | ||
| KP-N-YS | Growth inhibition assay | Inhibition of human KP-N-YS cell growth in a cell viability assay, IC50 = 42.0641 μM. | SANGER | ||
| T98G | Growth inhibition assay | Inhibition of human T98G cell growth in a cell viability assay, IC50 = 42.6733 μM. | SANGER | ||
| A431 | Growth inhibition assay | Inhibition of human A431 cell growth in a cell viability assay, IC50 = 45.1831 μM. | SANGER | ||
| HDLM-2 | Growth inhibition assay | Inhibition of human HDLM-2 cell growth in a cell viability assay, IC50 = 45.2617 μM. | SANGER | ||
| CHP-134 | Growth inhibition assay | Inhibition of human CHP-134 cell growth in a cell viability assay, IC50 = 46.1779 μM. | SANGER | ||
| J-RT3-T3-5 | Growth inhibition assay | Inhibition of human J-RT3-T3-5 cell growth in a cell viability assay, IC50 = 46.4461 μM. | SANGER | ||
| NCI-H1650 | Growth inhibition assay | Inhibition of human NCI-H1650 cell growth in a cell viability assay, IC50 = 46.5104 μM. | SANGER | ||
| MHH-PREB-1 | Growth inhibition assay | Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50 = 46.5266 μM. | SANGER | ||
| SJRH30 | Growth inhibition assay | Inhibition of human SJRH30 cell growth in a cell viability assay, IC50 = 46.7775 μM. | SANGER | ||
| SF295 | Growth inhibition assay | Inhibition of human SF295 cell growth in a cell viability assay, IC50 = 48.519 μM. | SANGER | ||
| YAPC | Growth inhibition assay | Inhibition of human YAPC cell growth in a cell viability assay, IC50 = 48.942 μM. | SANGER | ||
| EFM-19 | Growth inhibition assay | Inhibition of human EFM-19 cell growth in a cell viability assay, IC50 = 49.5085 μM. | SANGER | ||
| MIAPaCa2 | Proliferation assay | Antiproliferative activity against human MIAPaCa2 cells, IC50=142 nM. | 23474388 | ||
| A549 | Antiproliferative assay | Antiproliferative activity against human A549 cells, IC50 = 1.75 μM. | 23474388 | ||
| LoVo | Antiproliferative assay | Antiproliferative activity against human LoVo cells, IC50 = 2.83 μM. | 23474388 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells expressing KRAS G13D mutant, IC50 = 3.1 μM. | 23474388 | ||
| HeLa-MaTu | Function assay | Inhibition of MEK1 in human HeLa-MaTu matched pair cells assessed as reduction in ERK phosphorylation, IC50 = 0.014 μM. | 26611920 | ||
| HepG2 | Antiproliferative assay | Antiproliferative activity against human HepG2 cells harboring N-Ras mutation, IC50 = 0.032 μM. | 26611920 | ||
| COLO205 | Antiproliferative assay | Antiproliferative activity against human COLO205 cells harboring BRAF mutation, IC50 = 0.069 μM. | 26611920 | ||
| A549 | Antiproliferative assay | Antiproliferative activity against human A549 cells harboring K-Ras mutation, IC50 = 1.75 μM. | 26611920 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells harboring K-Ras G13D mutation, IC50 = 3 μM. | 26611920 | ||
| HeLa-MaTu-ADR | Function assay | Inhibition of MEK1 in human HeLa-MaTu-ADR matched pair cells assessed as reduction in ERK phosphorylation, IC50 = 3.7 μM. | 26611920 | ||
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生物活性
| 產品描述 | Selumetinib (AZD6244, ARRY-142886)是一種有效，高選擇性的MEK抑制劑，對MEK1的IC50為14 nM，對MEK2的Kd值為530 nM。它也抑制ERK1/2磷酸化，IC50為10 nM，對p38α， MKK6， EGFR， ErbB2， ERK2， B-Raf等沒有抑制作用。Selumetinib可抑制細胞增殖、遷移并誘導凋亡。Phase 3。 | ||||||
|---|---|---|---|---|---|---|---|
| 特性 | AZD6244是第一個處于隨機二期研究的MEK抑制劑。 | ||||||
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | AZD6244是ATP非競爭性的抑制劑，在IC50濃度小于40 nM時使ERK1/2的磷酸化作用失活。AZD6244也通過抑制ERK1/2和p90RSK的磷酸化抑制原代HCC細胞的生長，同時伴隨著caspase-3和caspase-7分裂的加強, 及斷裂的聚腺苷二磷酸核糖聚合酶的增多。AZD6244在P38，JNK，PI3K，及MEK5/ERK5通路中的作用不大。[1]AZD6244對感知乳腺癌細胞系中的raf突變和非小細胞肺癌細胞系中的ras突變很靈敏。[2] |
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|---|---|---|---|---|
| 激酶實驗 | 激酶實驗 | |||
| 在桿狀病毒感染的hi5昆蟲細胞中表達的組成型的氮端用六聚組氨酸標記的MEK1，通過金屬親和層析、離子交換及凝膠過濾純化。MEK1的活性評估通過測量[γ-33P]ATP 作用于ERK2的示蹤[γ-33P]磷酸的滲透率。實驗在96孔板中進行，保溫混合物由25 mM HEPES (pH 7.4), 10 mM MgCl2, 5 mM β-甘油磷酸 100 μM 原釩酸鈉, 5 mM DTT, 5 nM MEK1, 1 μM ERK2, 和AZD6244 (溶解在 1% DMSO)組成。加入10 μM ATP (0.5 μC k[γ-33P]ATP/每孔)反應開始，然后在室溫下溫育45分鐘。加入同等量的25%的三氯乙酸反應停止，使蛋白沉淀。沉淀的蛋白加到玻璃纖維過濾板上，用0.5%的磷酸沖洗掉過量的示蹤ATP，然后在液體閃爍計數(shù)管中計算放射性。通過在反應混合物中改變ATP的量來決定ATP相關性。 | ||||
| 細胞實驗 | 細胞系 | 原代HCC細胞系包括2-1318, 4-1318和26-1004細胞 | ||
| 濃度 | 10 μM 左右 | |||
| 孵育時間 | 24或48小時 | |||
| 方法 | 腫瘤細胞按2.0×104密度接種，溫育48小時，然后用培養(yǎng)基清洗細胞兩次。用不同濃度的AZD6244處理細胞24小時或者48小時。細胞活力通過MTT實驗來測定。用溴脫氧核苷尿嘧啶試劑盒測定細胞增殖。 |
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| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | p-ERK / ERK / β-catenin / E-cadherin / Vimentin / Fibronection pS6(235/236) / pS6(240/244) pVEGFR(Y1175) / VEGFR2 / pPDGFRβ(Y751) / pPDGFRβ / pAXL(Y702) / AXL / pMEK / MEK Bak / Bad / Bcl-xl / BimEL / BimL / BimS / PUMA / NOXA |
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26384399 | |
| Immunofluorescence | β-catenin FOXO3a |
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26384399 | |
| Growth inhibition assay | Cell viability |
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26384399 | |
| 體內研究(In Vivo) | ||
| 體內研究活性 | 活體研究顯示AZD6244在2-1318, 5-1318, 及26-1004 4-1318移植物中明顯抑制ERK1/2的磷酸化，并且在原代2-1318細胞中通過激活caspase通路誘導細胞凋亡。[1]HT-29移植瘤是攜帶B-raf突變的直腸瘤模型，AZD6244 在100mg/kg劑量時可以抑制HT-29移植瘤中腫瘤的增長，并且AZD6244作用下的腫瘤指數(shù)比吉西他濱作用下的腫瘤指數(shù)要好[3]。另外，AZD6244可以抑制HCC移植瘤的增長，HCC移植瘤的增長與細胞凋亡的增多，及細胞周期調控的減量調節(jié)有關。包括：cyclin D1, cdc-2, CDK 2 ,CDK4, cyclin B1, 及 c-Myc。[4] |
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|---|---|---|
| 動物實驗 | Animal Models | 攜帶HCC移植瘤的SCID鼠 |
| Dosages | 50或100mg/kg | |
| Administration | 口服處理 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05253131 | Not yet recruiting | MPNST|NF1|Sarcoma |
University of Alabama at Birmingham|United States Department of Defense |
June 15 2024 | Phase 2 |
| NCT06175637 | Recruiting | Neurofibroma Plexiform |
AstraZeneca |
December 20 2023 | -- |
| NCT05891847 | Recruiting | Neurofibroma |
AstraZeneca |
March 21 2023 | -- |
| NCT05101148 | Active not recruiting | Neurofibromatosis Type 1 |
AstraZeneca|Merck Sharp & Dohme LLC |
July 21 2021 | Phase 1 |
| NCT04879160 | Completed | Neurofibromatosis 1 |
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
May 12 2021 | -- |
化學信息&溶解度
| 分子量 | 457.68 | 分子式 | C17H15BrClFN4O3 |
| CAS號 | 606143-52-6 | SDF | Download Selumetinib (AZD6244) SDF |
| Smiles | CN1C=NC2=C1C=C(C(=C2F)NC3=C(C=C(C=C3)Br)Cl)C(=O)NOCCO | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 91 mg/mL ( (198.82 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內配方計算器 | ||||
實驗計算
動物體內配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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常見問題及建議解決方法
問題 1:
How about the solubility of S1008? How to prepare for the solution if I need to do the in vivo experiments?
回答：
S1008 AZD6244 in vehicle 5% DMSO+30% PEG 300+ddH2O will be a suspension for oral administration. If you want a clear solution for injection, you can dissolve it in 4% DMSO+30% PEG 300+5% Tween 80+ddH2O.
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