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PLX-4720
PLX-4720是一種有效的，選擇性的B-RafV600E抑制劑，無細胞試驗中IC50為13 nM，同樣有效地作用于c-Raf-1(Y340D和Y341D突變型)，作用于B-RafV600E比作用于野生型B-Raf選擇性高10倍。
PLX-4720 Chemical Structure
CAS: 918505-84-7
產(chǎn)品質(zhì)控
批次：
純度：
99.98%
99.98
常與PLX-4720一起在實驗中被使用的化合物
PLX-4720和Dactolisib治療可降低Colo-205異種移植物中的pERK和pAKT水平。
Schulte ML, et al. Mol Imaging Biol. 2017 Jun;19(3):421-428.
PLX-4720和Navitoclax可以增強BRAF抑制劑的臨床療效。
Frederick DT, et al. Cancer Res (2013) 73 (8_Supplement): 1724.
PLX-4720和Dabrafenib可顯著減少BRAF突變黑色素瘤細胞因腦脊液存在而死亡。
Seifert H, et al. Pigment Cell Melanoma Res. 2016 Jan;29(1):92-100.
PLX-4720和NMS-E973在A375黑色素瘤細胞中顯示出協(xié)同抗增殖活性。
Fogliatto G, et al. Clin Cancer Res. 2013 Jul 1;19(13):3520-32.
PLX-4720和SB431542共處理消除了低劑量PLX-4720在Colo829和A375(M2)細胞中引起的細胞生長增加。
Spender LC, et al. Oncotarget. 2016 Dec 13; 7(50): 81995–82012.
PLX-4720相關(guān)產(chǎn)品
相關(guān)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 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 72 hrs by CellTiter-Glo assay, IC50 = 0.5 μM. | 29461827 | |
| SK-LU-1 | Growth Inhibition Assay | IC50=12.2655 μM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=11.7178 μM | SANGER | ||
| SK-HEP-1 | Growth Inhibition Assay | IC50=11.3527 μM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=11.2404 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=10.8472 μM | SANGER | ||
| SK-MEL-24 | Growth Inhibition Assay | IC50=10.8274 μM | SANGER | ||
| LXF-289 | Growth Inhibition Assay | IC50=10.458 μM | SANGER | ||
| A431 | Growth Inhibition Assay | IC50=10.4212 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=10.0149 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=9.6048 μM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=9.56999 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=9.05178 μM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=8.75314 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=8.41516 μM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=8.07068 μM | SANGER | ||
| COLO-741 | Growth Inhibition Assay | IC50=8.01679 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=7.36907 μM | SANGER | ||
| BCPAP | Growth Inhibition Assay | IC50=7.21764 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=6.81931 μM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=6.45423 μM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=6.22493 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=6.21373 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=6.18129 μM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=6.14924 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=6.10946 μM | SANGER | ||
| TI-73 | Growth Inhibition Assay | IC50=6.00902 μM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=5.97603 μM | SANGER | ||
| RPMI-7951 | Growth Inhibition Assay | IC50=5.80283 μM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=5.1873 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=4.73908 μM | SANGER | ||
| A2058 | Growth Inhibition Assay | IC50=4.72164 μM | SANGER | ||
| DBTRG-05MG | Growth Inhibition Assay | IC50=4.53325 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=4.49179 μM | SANGER | ||
| CP66-MEL | Growth Inhibition Assay | IC50=4.15927 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=3.55266 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=3.40176 μM | SANGER | ||
| NCI-H358 | Growth Inhibition Assay | IC50=2.92232 μM | SANGER | ||
| HuO-3N1 | Growth Inhibition Assay | IC50=2.87946 μM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=2.72673 μM | SANGER | ||
| KP-4 | Growth Inhibition Assay | IC50=2.30787 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=2.11969 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=2.04978 μM | SANGER | ||
| HTC-C3 | Growth Inhibition Assay | IC50=1.66294 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=1.6086 μM | SANGER | ||
| SK-MEL-30 | Growth Inhibition Assay | IC50=1.33386 μM | SANGER | ||
| MZ7-mel | Growth Inhibition Assay | IC50=1.14963 μM | SANGER | ||
| COLO-679 | Growth Inhibition Assay | IC50=1.10464 μM | SANGER | ||
| SK-MEL-28 | Growth Inhibition Assay | IC50=1.04569 μM | SANGER | ||
| WM-115 | Growth Inhibition Assay | IC50=0.88692 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=0.87844 μM | SANGER | ||
| RVH-421 | Growth Inhibition Assay | IC50=0.86796 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=0.79644 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=0.76148 μM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=0.70702 μM | SANGER | ||
| MMAC-SF | Growth Inhibition Assay | IC50=0.68614 μM | SANGER | ||
| A375 | Growth Inhibition Assay | IC50=0.67359 μM | SANGER | ||
| SK-MEL-3 | Growth Inhibition Assay | IC50=0.51568 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=0.41422 μM | SANGER | ||
| MEL-HO | Growth Inhibition Assay | IC50=0.41179 μM | SANGER | ||
| COLO-829 | Growth Inhibition Assay | IC50=0.38968 μM | SANGER | ||
| ACN | Growth Inhibition Assay | IC50=0.38477 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=0.36329 μM | SANGER | ||
| G-361 | Growth Inhibition Assay | IC50=0.34637 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=0.32589 μM | SANGER | ||
| CP50-MEL-B | Growth Inhibition Assay | IC50=0.29784 μM | SANGER | ||
| M14 | Growth Inhibition Assay | IC50=0.21757 μM | SANGER | ||
| C32 | Growth Inhibition Assay | IC50=0.15131 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.14166 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=0.07457 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=12.3932 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=12.6062 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=12.7169 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=12.8833 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=13.9576 μM | SANGER | ||
| KYSE-140 | Growth Inhibition Assay | IC50=14.0753 μM | SANGER | ||
| SCC-4 | Growth Inhibition Assay | IC50=14.3359 μM | SANGER | ||
| U251 | Growth Inhibition Assay | IC50=14.8492 μM | SANGER | ||
| D-542MG | Growth Inhibition Assay | IC50=14.9222 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=14.9932 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=15.2684 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=15.4293 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=15.4305 μM | SANGER | ||
| ECC10 | Growth Inhibition Assay | IC50=15.4458 μM | SANGER | ||
| Daoy | Growth Inhibition Assay | IC50=15.7616 μM | SANGER | ||
| SCH | Growth Inhibition Assay | IC50=15.7835 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=16.0646 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=16.4862 μM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=16.8107 μM | SANGER | ||
| LS-411N | Growth Inhibition Assay | IC50=17.118 μM | SANGER | ||
| NCI-H2228 | Growth Inhibition Assay | IC50=17.3071 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=17.4965 μM | SANGER | ||
| HN | Growth Inhibition Assay | IC50=17.7248 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=17.818 μM | SANGER | ||
| IA-LM | Growth Inhibition Assay | IC50=18.3172 μM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=18.5708 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=19.5711 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=19.5858 μM | SANGER | ||
| 23132-87 | Growth Inhibition Assay | IC50=19.7642 μM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=19.9887 μM | SANGER | ||
| 5637 | Growth Inhibition Assay | IC50=20.0478 μM | SANGER | ||
| NCI-H1755 | Growth Inhibition Assay | IC50=20.4764 μM | SANGER | ||
| RH-18 | Growth Inhibition Assay | IC50=20.5748 μM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=20.6756 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=20.7056 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=20.7201 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=21.1915 μM | SANGER | ||
| IGR-1 | Growth Inhibition Assay | IC50=21.3796 μM | SANGER | ||
| HOP-92 | Growth Inhibition Assay | IC50=21.4987 μM | SANGER | ||
| SK-MES-1 | Growth Inhibition Assay | IC50=21.7381 μM | SANGER | ||
| LU-65 | Growth Inhibition Assay | IC50=21.8624 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=22.1203 μM | SANGER | ||
| LoVo | Growth Inhibition Assay | IC50=22.244 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=22.5155 μM | SANGER | ||
| HT-1376 | Growth Inhibition Assay | IC50=22.6059 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=22.6751 μM | SANGER | ||
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=22.7366 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=22.7979 μM | SANGER | ||
| HT-1197 | Growth Inhibition Assay | IC50=23.0817 μM | SANGER | ||
| LB2518-MEL | Growth Inhibition Assay | IC50=23.6412 μM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=24.7595 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=24.8744 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=25.0023 μM | SANGER | ||
| IST-SL1 | Growth Inhibition Assay | IC50=25.2751 μM | SANGER | ||
| HH | Growth Inhibition Assay | IC50=25.3192 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=25.938 μM | SANGER | ||
| SNU-449 | Growth Inhibition Assay | IC50=27.2018 μM | SANGER | ||
| COR-L23 | Growth Inhibition Assay | IC50=27.2813 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=27.368 μM | SANGER | ||
| GR-ST | Growth Inhibition Assay | IC50=27.6706 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=27.944 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=28.1604 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=28.2814 μM | SANGER | ||
| HOP-62 | Growth Inhibition Assay | IC50=28.713 μM | SANGER | ||
| EGI-1 | Growth Inhibition Assay | IC50=28.8845 μM | SANGER | ||
| TCCSUP | Growth Inhibition Assay | IC50=28.9272 μM | SANGER | ||
| LB996-RCC | Growth Inhibition Assay | IC50=29.5682 μM | SANGER | ||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=32.1964 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=32.3301 μM | SANGER | ||
| KP-N-YS | Growth Inhibition Assay | IC50=32.5973 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=33.1648 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=33.6504 μM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=33.7236 μM | SANGER | ||
| ACHN | Growth Inhibition Assay | IC50=33.8385 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=33.8544 μM | SANGER | ||
| EW-18 | Growth Inhibition Assay | IC50=33.8971 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=35.7292 μM | SANGER | ||
| U031 | Growth Inhibition Assay | IC50=35.8132 μM | SANGER | ||
| HMV-II | Growth Inhibition Assay | IC50=36.0774 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=37.6455 μM | SANGER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=38.0015 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=38.1026 μM | SANGER | ||
| P30-OHK | Growth Inhibition Assay | IC50=38.1332 μM | SANGER | ||
| AN3-CA | Growth Inhibition Assay | IC50=38.1615 μM | SANGER | ||
| UACC-257 | Growth Inhibition Assay | IC50=38.79 μM | SANGER | ||
| MCF7 | Growth Inhibition Assay | IC50=39.8629 μM | SANGER | ||
| KP-N-YN | Growth Inhibition Assay | IC50=40.4285 μM | SANGER | ||
| T98G | Growth Inhibition Assay | IC50=40.4957 μM | SANGER | ||
| HGC-27 | Growth Inhibition Assay | IC50=43.274 μM | SANGER | ||
| NCI-H1092 | Growth Inhibition Assay | IC50=43.2895 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=43.3071 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=44.9959 μM | SANGER | ||
| 786-0 | Growth Inhibition Assay | IC50=45.65 μM | SANGER | ||
| HCC2157 | Growth Inhibition Assay | IC50=46.0359 μM | SANGER | ||
| NY | Growth Inhibition Assay | IC50=46.1778 μM | SANGER | ||
| EFM-19 | Growth Inhibition Assay | IC50=46.7533 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=46.7806 μM | SANGER | ||
| UM-UC-3 | Growth Inhibition Assay | IC50=46.8059 μM | SANGER | ||
| HT-29 | Growth Inhibition Assay | IC50=47.8792 μM | SANGER | ||
| LN-405 | Growth Inhibition Assay | IC50=48.0827 μM | SANGER | ||
| NCI-H727 | Growth Inhibition Assay | IC50=48.7726 μM | SANGER | ||
| D-502MG | Growth Inhibition Assay | IC50=48.9676 μM | SANGER | ||
| GMS-10 | Growth Inhibition Assay | IC50=49.2974 μM | SANGER | ||
| MEL-JUSO | Growth Inhibition Assay | IC50=49.347 μM | SANGER | ||
| insect cells | Function assay | Inhibition of N-terminal His-tagged BRAF V600E mutant (unknown origin) expressed in baculovirus infected insect cells co-expressing CDC37 using biotinylated-MEK as substrate by AlphaScreen assay, IC50 = 0.013 μM. | 29461827 | ||
| A375 | Function assay | Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in ERK phosphorylation by AlphaScreen assay, IC50 = 0.044 μM. | 29461827 | ||
| A375 | Function assay | Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK, IC50 = 0.046 μM. | 22808911 | ||
| A375 | Antiproliferative assay | Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras, IC50 = 0.5 μM. | 22808911 | ||
| HCT116 | Antiproliferative assay | Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant, IC50 = 27 μM. | 22808911 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | PLX-4720是一種有效的，選擇性的B-RafV600E抑制劑，無細胞試驗中IC50為13 nM，同樣有效地作用于c-Raf-1(Y340D和Y341D突變型)，作用于B-RafV600E比作用于野生型B-Raf選擇性高10倍。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | PLX-4720高親和力與活性B-RafV600E和c-Raf-1Y340D/Y341D結(jié)合，作用于野生型B-Raf選擇性>10倍,作用于其他激酶如Frk, Src, Fak, FGFR, 和Aurora A 選擇性>100倍，IC50為1.3-3.4 μM。與有效的選擇性相一致, PLX-4720作用于攜帶B-RafV600E的細胞系，顯著抑制ERK磷酸化，IC50為14-46 nM, 但是對攜帶野生型B-Raf的細胞沒有作用效果。PLX-4720 作用于攜帶B-RafV600E致癌基因（如COLO205, A375, WM2664, 和 COLO829）的腫瘤細胞系，顯著抑制細胞生長，GI50 分別為 0.31 μM, 0.50 μM, 1.5 μM, 和 1.7 μM。此外, 1 μM PLX-4720 只有作用于B-RafV600E-陽性1205Lu細胞, 誘導(dǎo)細胞周期停滯和凋亡，而作用于B-Raf 野生型C8161細胞則無此效果。[1]10 μM PLX-4720 處理PTEN+細胞，誘導(dǎo)BIM表達，比PTEN-細胞系(4倍-fold)高14倍，說明PTEN-細胞系抗PLX-4720誘導(dǎo)的凋亡。[2] | |||
|---|---|---|---|---|
| 激酶實驗 | 體外Raf激酶活性實驗 | |||
| 通過測量生物素-MEK蛋白，使用Perkin-Elmer's AlphaScreen 技術(shù)測定體外野生型和突變型Raf的激酶活性。在20 mM Hepes (pH 7.0), 10 mM MgCl2, 1 mM DTT, 0.01% Tween-20, 100 nM 生物素-MEK 蛋白,多種ATP濃度,及濃度不斷增高的PLX-4720混合物中在室溫下進行每組酶(0.1 ng)反應(yīng)，反應(yīng)體積為20-μL。 在 2, 5, 8, 10, 20,和 30分鐘加入5 μL含20 mM Hepes (pH 7.0), 200 mM NaCl, 80 mM EDTA, 和 0.3% BSA的溶液終止反應(yīng)。終止液包括磷酸-MEK抗體, 鏈霉親和素包被的供體珠，和AlphaScreen蛋白 A檢測試劑盒中的蛋白A受體珠?？贵w和小株在終止液中在室溫下黑暗溫育30分鐘?？贵w最終按 1:2,000稀釋,每個小珠終濃度為 10 μg/mL。實驗板在室溫下溫育1小時，然后在 PerkinElmer AlphaQuest 讀數(shù)器上讀數(shù)。 | ||||
| 細胞實驗 | 細胞系 | COLO205, A375, WM2664, COLO829, HT716, SW620, H460, Calu-6, HCT116, SK-MEL2, SK-MEL3, Lovo, H1299, 1205Lu, 和C8161 | ||
| 濃度 | 溶于DMSO, 終濃度為~1 mM | |||
| 孵育時間 | 24, 48, 和 72小時 | |||
| 方法 | 使用不同濃度PLX-4720 for處理細胞 24, 48,和72小時通過 CellTiter-GLO熒光細胞活性檢測或MTT實驗測定細胞增殖。為了分析細胞周期, 收集上清液和細胞, 制成顆粒，與70%乙醇混合。在使用碘化丙啶 (10 μg/mL)染色前,細胞在0.5 mg/mL RNase I 中37oC下溫育1小時，除去殘留RNA污染樣本。使用EPICS XL儀分析樣本。為了測定凋亡, 獲得培養(yǎng)基和細胞，制成顆粒，然后使用膜聯(lián)蛋白-FITC和碘化丙啶染色。然后再使用EPICS XL儀分析樣本。 | |||
| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
| Western blot | pAkt(Ser473) / pAkt(Thr308) p27 / Cyclin D1 / pRb p-EGFR 1173 / EGFR / p-Akt / Akt p-MEK / MEK / p-ERK / ERK / p-FAK(S910) |
|
21828154 | |
| Immunofluorescence | ZKSCAN3 / TFEB LAMP1 |
|
30979895 | |
| Growth inhibition assay | Cell viability |
|
27848137 | |
| ELISA | mIFN-γ |
|
23204132 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | PLX-4720每天按20 mg/kg劑量口服給藥依賴B-RafV600E的COLO205移植瘤，顯著延遲腫瘤生長，且引起腫瘤衰退, 即使按1 g/kg劑量處理也不會對小鼠造成明顯的不利影響。PLX-4720按 100 mg/kg劑量處理 攜帶B-RafV600E的1205Lu 移植瘤，每天兩次，幾乎完全消除腫瘤, 而對攜帶野生型B-Raf的C8161 移植瘤則沒有作用活性。PLX-4720 作用于含V600E突變細胞的抗癌效果與阻斷MAPK通路相關(guān)。[1] PLX-4720每天按30 mg/kg劑量處理8505c腫瘤，顯著抑制腫瘤生長，抑制達90%以上,也顯著降低遠處肺轉(zhuǎn)移。[3] | |
|---|---|---|
| 動物實驗 | Animal Models | 皮下移植 COLO205 細胞的雌性無胸腺NCr nu/nu小鼠, 攜帶1205Lu或C8161 細胞的SCID小鼠 |
| Dosages | 5, 20, 或100 mg/kg | |
| Administration | 口服飼喂，每天一次或兩次 | |
化學(xué)信息&溶解度
| 分子量 | 413.83 | 分子式 | C17H14ClF2N3O3S |
| CAS號 | 918505-84-7 | SDF | Download PLX-4720 SDF |
| Smiles | CCCS(=O)(=O)NC1=C(C(=C(C=C1)F)C(=O)C2=CNC3=C2C=C(C=N3)Cl)F | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 83 mg/mL ( (200.56 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(nèi)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(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)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(nèi)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(jié)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(nèi)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(nèi)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。
技術(shù)支持
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如果有其他問題，請給我們留言。
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常見問題及建議解決方法
問題 1:
What would you recommend to make working solution for intraperitoneal injection into mice?
回答：
PLX4720 has very limited solubility in aqueous solution and for this reason, we recommend oral gavage to administer this compound as not fully dissolved suspension can be used in oral gavage feeding.
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