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Angiogenesis
Src inhibitor
-
ERK inhibitor
-
S6 Kinase inhibitor
-
STAT inhibitor
-
Bcr-Abl inhibitor
-
Autophagy activator
Bosutinib
僅限科研使用
Bosutinib
別名: SKI-606 中文名稱：伯舒替尼
Bosutinib是一種新型的雙重Src/Abl抑制劑，在無細(xì)胞試驗(yàn)中IC50分別為1.2 nM 和 1 nM。Bosutinib也可通過阻滯p-ERK、p-S6和p-STAT3的磷酸化來有效地降低PI3K/AKT/mTOR、MAPK/ERK和JAK/STAT3信號通路的活性。Bosutinib可促進(jìn)自噬。
Bosutinib Chemical Structure
CAS: 380843-75-4
產(chǎn)品質(zhì)控
批次：
純度：
99.94%
99.94
Bosutinib相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | Lck Fyn Lyn Yes Fgr | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Saracatinib (AZD0530) PP2 SU6656 PP1 WH-4-023 Src Inhibitor 1 RK 24466 Myristic Acid eCF506 Tolimidone (MLR-1023) UM-164 | 點(diǎn)擊展開 |
| 相關(guān)化合物庫 | 酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫 血管生成相關(guān)化合物庫 HIF-1信號通路化合物庫 FDA抗癌藥物庫 | 點(diǎn)擊展開 |
相關(guān)信號通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息 |
|---|---|---|---|---|---|
| K562 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.0043 μM. | 26814890 | |
| HEK293 | Function assay | 1 hr | Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, Ki = 0.0127 μM. | 29941193 | |
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E355G mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.128 μM. | 30137981 | |
| HEK293 | Function assay | 1 hr | Inhibition of human full length PKMYT1 expressed in HEK293 cells using EFS (247 to 259 residues) as substrate after 1 hr by fluorescence polarization immunoasay, IC50 = 0.133 μM. | 29941193 | |
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E459K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.14 μM. | 30137981 | |
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 G250H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.146 μM. | 30137981 | |
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 Y253H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.177 μM. | 30137981 | |
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 F359V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.195 μM. | 30137981 | |
| Ba/F3 | Function assay | 48 hrs | Inhibition of wild type BCR-ABL1 (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.204 μM. | 30137981 | |
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 Q252H mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.243 μM. | 30137981 | |
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E255V mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.278 μM. | 30137981 | |
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 E255K mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of BCR-ABL1-mediated cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.356 μM. | 30137981 | |
| Ba/F3 | Function assay | 48 hrs | Inhibition of BCR-ABL1 T315I mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as inhibition of cell proliferation after 48 hrs by BriteLight luciferase assay, GI50 = 0.642 μM. | 30137981 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay, GI50 = 1.15 μM. | 18485715 | |
| HT29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay, GI50 = 1.17 μM. | 18485715 | |
| BA/F3 | Cytotoxicity assay | 72 hrs | Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay, IC50 = 3.2 μM. | 26814890 | |
| HeLa | Function assay | 4.5 hrs | Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay, IC50 = 3.85 μM. | 29624387 | |
| HT29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay, IC50 = 3.87 μM. | 18485715 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay, IC50 = 3.91 μM. | 18485715 | |
| HT29 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HT29 cells after 48 hrs by sulforhodamine B assay, TGI = 6.5 μM. | 18485715 | |
| HepG2 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HepG2 cells after 48 hrs by sulforhodamine B assay, TGI = 7.66 μM. | 18485715 | |
| Ramos-2G6-4C10 | Growth Inhibition Assay | IC50=4.16739 μM | SANGER | ||
| MN-60 | Growth Inhibition Assay | IC50=4.10501 μM | SANGER | ||
| KYSE-520 | Growth Inhibition Assay | IC50=4.09799 μM | SANGER | ||
| Mewo | Growth Inhibition Assay | IC50=4.06361 μM | SANGER | ||
| U-266 | Growth Inhibition Assay | IC50=3.97481 μM | SANGER | ||
| MIA-PaCa-2 | Growth Inhibition Assay | IC50=3.9729 μM | SANGER | ||
| KYSE-450 | Growth Inhibition Assay | IC50=3.96997 μM | SANGER | ||
| NCI-H1755 | Growth Inhibition Assay | IC50=3.96971 μM | SANGER | ||
| HuCCT1 | Growth Inhibition Assay | IC50=3.74177 μM | SANGER | ||
| BT-549 | Growth Inhibition Assay | IC50=3.67854 μM | SANGER | ||
| NOS-1 | Growth Inhibition Assay | IC50=3.64276 μM | SANGER | ||
| DSH1 | Growth Inhibition Assay | IC50=3.64122 μM | SANGER | ||
| SW982 | Growth Inhibition Assay | IC50=3.58829 μM | SANGER | ||
| H-EMC-SS | Growth Inhibition Assay | IC50=3.58569 μM | SANGER | ||
| NCI-H1650 | Growth Inhibition Assay | IC50=3.5729 μM | SANGER | ||
| NCI-H1792 | Growth Inhibition Assay | IC50=3.49802 μM | SANGER | ||
| MOLT-4 | Growth Inhibition Assay | IC50=3.48199 μM | SANGER | ||
| A427 | Growth Inhibition Assay | IC50=3.46124 μM | SANGER | ||
| NCI-H1703 | Growth Inhibition Assay | IC50=3.41812 μM | SANGER | ||
| C-33-A | Growth Inhibition Assay | IC50=3.41421 μM | SANGER | ||
| SCH | Growth Inhibition Assay | IC50=3.40844 μM | SANGER | ||
| GMS-10 | Growth Inhibition Assay | IC50=3.34086 μM | SANGER | ||
| NCI-N87 | Growth Inhibition Assay | IC50=3.30172 μM | SANGER | ||
| HL-60 | Growth Inhibition Assay | IC50=3.2913 μM | SANGER | ||
| NCI-H2009 | Growth Inhibition Assay | IC50=3.2901 μM | SANGER | ||
| ME-180 | Growth Inhibition Assay | IC50=3.26051 μM | SANGER | ||
| SW48 | Growth Inhibition Assay | IC50=3.25486 μM | SANGER | ||
| SK-MES-1 | Growth Inhibition Assay | IC50=3.24829 μM | SANGER | ||
| HSC-2 | Growth Inhibition Assay | IC50=3.22232 μM | SANGER | ||
| T-24 | Growth Inhibition Assay | IC50=3.21814 μM | SANGER | ||
| P30-OHK | Growth Inhibition Assay | IC50=3.20117 μM | SANGER | ||
| SK-LU-1 | Growth Inhibition Assay | IC50=3.18418 μM | SANGER | ||
| EC-GI-10 | Growth Inhibition Assay | IC50=3.17263 μM | SANGER | ||
| YKG-1 | Growth Inhibition Assay | IC50=3.14706 μM | SANGER | ||
| EW-11 | Growth Inhibition Assay | IC50=3.14277 μM | SANGER | ||
| 8505C | Growth Inhibition Assay | IC50=3.10301 μM | SANGER | ||
| EPLC-272H | Growth Inhibition Assay | IC50=3.00235 μM | SANGER | ||
| SAS | Growth Inhibition Assay | IC50=2.99415 μM | SANGER | ||
| SK-MEL-2 | Growth Inhibition Assay | IC50=2.89243 μM | SANGER | ||
| OMC-1 | Growth Inhibition Assay | IC50=2.85003 μM | SANGER | ||
| SK-N-DZ | Growth Inhibition Assay | IC50=2.81638 μM | SANGER | ||
| MHH-PREB-1 | Growth Inhibition Assay | IC50=2.80161 μM | SANGER | ||
| COR-L23 | Growth Inhibition Assay | IC50=2.79464 μM | SANGER | ||
| SK-MEL-24 | Growth Inhibition Assay | IC50=2.78224 μM | SANGER | ||
| OS-RC-2 | Growth Inhibition Assay | IC50=2.76673 μM | SANGER | ||
| SF295 | Growth Inhibition Assay | IC50=2.7431 μM | SANGER | ||
| RPMI-8226 | Growth Inhibition Assay | IC50=2.73164 μM | SANGER | ||
| SK-UT-1 | Growth Inhibition Assay | IC50=2.71406 μM | SANGER | ||
| MSTO-211H | Growth Inhibition Assay | IC50=2.66391 μM | SANGER | ||
| L-363 | Growth Inhibition Assay | IC50=2.43507 μM | SANGER | ||
| DB | Growth Inhibition Assay | IC50=2.42869 μM | SANGER | ||
| CAL-12T | Growth Inhibition Assay | IC50=2.40417 μM | SANGER | ||
| TE-11 | Growth Inhibition Assay | IC50=2.38019 μM | SANGER | ||
| A431 | Growth Inhibition Assay | IC50=2.37025 μM | SANGER | ||
| FADU | Growth Inhibition Assay | IC50=2.32296 μM | SANGER | ||
| TYK-nu | Growth Inhibition Assay | IC50=2.30909 μM | SANGER | ||
| HTC-C3 | Growth Inhibition Assay | IC50=2.26824 μM | SANGER | ||
| HCT-116 | Growth Inhibition Assay | IC50=2.22984 μM | SANGER | ||
| NCI-H2030 | Growth Inhibition Assay | IC50=2.18973 μM | SANGER | ||
| CAL-39 | Growth Inhibition Assay | IC50=2.1448 μM | SANGER | ||
| TK10 | Growth Inhibition Assay | IC50=2.13458 μM | SANGER | ||
| NBsusSR | Growth Inhibition Assay | IC50=2.09889 μM | SANGER | ||
| MOLT-16 | Growth Inhibition Assay | IC50=2.07058 μM | SANGER | ||
| MEL-JUSO | Growth Inhibition Assay | IC50=2.04464 μM | SANGER | ||
| C2BBe1 | Growth Inhibition Assay | IC50=2.03372 μM | SANGER | ||
| SK-HEP-1 | Growth Inhibition Assay | IC50=2.00745 μM | SANGER | ||
| OVCAR-4 | Growth Inhibition Assay | IC50=2.00435 μM | SANGER | ||
| NCI-H1693 | Growth Inhibition Assay | IC50=1.99888 μM | SANGER | ||
| NCI-H526 | Growth Inhibition Assay | IC50=1.99325 μM | SANGER | ||
| LoVo | Growth Inhibition Assay | IC50=1.97679 μM | SANGER | ||
| A101D | Growth Inhibition Assay | IC50=1.93628 μM | SANGER | ||
| HN | Growth Inhibition Assay | IC50=1.89874 μM | SANGER | ||
| BB65-RCC | Growth Inhibition Assay | IC50=1.89849 μM | SANGER | ||
| ES5 | Growth Inhibition Assay | IC50=1.86747 μM | SANGER | ||
| KYSE-140 | Growth Inhibition Assay | IC50=1.75655 μM | SANGER | ||
| LOXIMVI | Growth Inhibition Assay | IC50=1.74599 μM | SANGER | ||
| NKM-1 | Growth Inhibition Assay | IC50=1.71802 μM | SANGER | ||
| MV-4-11 | Growth Inhibition Assay | IC50=1.69856 μM | SANGER | ||
| 769-P | Growth Inhibition Assay | IC50=1.69596 μM | SANGER | ||
| EFO-27 | Growth Inhibition Assay | IC50=1.6892 μM | SANGER | ||
| ONS-76 | Growth Inhibition Assay | IC50=1.67551 μM | SANGER | ||
| CAL-54 | Growth Inhibition Assay | IC50=1.65709 μM | SANGER | ||
| HT-1376 | Growth Inhibition Assay | IC50=1.6436 μM | SANGER | ||
| HD-MY-Z | Growth Inhibition Assay | IC50=1.63584 μM | SANGER | ||
| SCC-15 | Growth Inhibition Assay | IC50=1.61804 μM | SANGER | ||
| D-566MG | Growth Inhibition Assay | IC50=1.57155 μM | SANGER | ||
| Ca9-22 | Growth Inhibition Assay | IC50=1.5626 μM | SANGER | ||
| SW954 | Growth Inhibition Assay | IC50=1.55007 μM | SANGER | ||
| A375 | Growth Inhibition Assay | IC50=1.51772 μM | SANGER | ||
| J-RT3-T3-5 | Growth Inhibition Assay | IC50=1.51722 μM | SANGER | ||
| JAR | Growth Inhibition Assay | IC50=1.4936 μM | SANGER | ||
| BPH-1 | Growth Inhibition Assay | IC50=1.44805 μM | SANGER | ||
| EW-16 | Growth Inhibition Assay | IC50=1.43973 μM | SANGER | ||
| DEL | Growth Inhibition Assay | IC50=1.43657 μM | SANGER | ||
| KG-1 | Growth Inhibition Assay | IC50=1.41273 μM | SANGER | ||
| A498 | Growth Inhibition Assay | IC50=1.40113 μM | SANGER | ||
| KOSC-2 | Growth Inhibition Assay | IC50=1.31775 μM | SANGER | ||
| MHH-NB-11 | Growth Inhibition Assay | IC50=1.31383 μM | SANGER | ||
| A4-Fuk | Growth Inhibition Assay | IC50=1.30704 μM | SANGER | ||
| NUGC-3 | Growth Inhibition Assay | IC50=1.29356 μM | SANGER | ||
| PC-14 | Growth Inhibition Assay | IC50=1.29205 μM | SANGER | ||
| BB30-HNC | Growth Inhibition Assay | IC50=1.28714 μM | SANGER | ||
| HO-1-N-1 | Growth Inhibition Assay | IC50=1.26369 μM | SANGER | ||
| RPMI-8866 | Growth Inhibition Assay | IC50=1.26106 μM | SANGER | ||
| H4 | Growth Inhibition Assay | IC50=1.24255 μM | SANGER | ||
| LB1047-RCC | Growth Inhibition Assay | IC50=1.23785 μM | SANGER | ||
| BHY | Growth Inhibition Assay | IC50=1.22892 μM | SANGER | ||
| ES4 | Growth Inhibition Assay | IC50=1.2079 μM | SANGER | ||
| CAL-33 | Growth Inhibition Assay | IC50=1.19302 μM | SANGER | ||
| 5637 | Growth Inhibition Assay | IC50=1.13803 μM | SANGER | ||
| KY821 | Growth Inhibition Assay | IC50=1.13351 μM | SANGER | ||
| HSC-3 | Growth Inhibition Assay | IC50=1.11783 μM | SANGER | ||
| QIMR-WIL | Growth Inhibition Assay | IC50=1.09058 μM | SANGER | ||
| HAL-01 | Growth Inhibition Assay | IC50=1.0881 μM | SANGER | ||
| JVM-3 | Growth Inhibition Assay | IC50=1.05017 μM | SANGER | ||
| TI-73 | Growth Inhibition Assay | IC50=1.0165 μM | SANGER | ||
| COR-L105 | Growth Inhibition Assay | IC50=1.00394 μM | SANGER | ||
| SK-NEP-1 | Growth Inhibition Assay | IC50=0.97248 μM | SANGER | ||
| CAL-27 | Growth Inhibition Assay | IC50=0.92906 μM | SANGER | ||
| KARPAS-45 | Growth Inhibition Assay | IC50=0.92466 μM | SANGER | ||
| MLMA | Growth Inhibition Assay | IC50=0.90675 μM | SANGER | ||
| OC-314 | Growth Inhibition Assay | IC50=0.86965 μM | SANGER | ||
| LB771-HNC | Growth Inhibition Assay | IC50=0.83104 μM | SANGER | ||
| A3-KAW | Growth Inhibition Assay | IC50=0.79208 μM | SANGER | ||
| SW13 | Growth Inhibition Assay | IC50=0.73798 μM | SANGER | ||
| KASUMI-1 | Growth Inhibition Assay | IC50=0.7233 μM | SANGER | ||
| ES1 | Growth Inhibition Assay | IC50=0.67498 μM | SANGER | ||
| EW-3 | Growth Inhibition Assay | IC50=0.55935 μM | SANGER | ||
| CHL-1 | Growth Inhibition Assay | IC50=0.55465 μM | SANGER | ||
| HT-1080 | Growth Inhibition Assay | IC50=0.55349 μM | SANGER | ||
| CTB-1 | Growth Inhibition Assay | IC50=0.5482 μM | SANGER | ||
| ACHN | Growth Inhibition Assay | IC50=0.54069 μM | SANGER | ||
| LB2241-RCC | Growth Inhibition Assay | IC50=0.53718 μM | SANGER | ||
| MEG-01 | Growth Inhibition Assay | IC50=0.51214 μM | SANGER | ||
| BV-173 | Growth Inhibition Assay | IC50=0.50792 μM | SANGER | ||
| KE-37 | Growth Inhibition Assay | IC50=0.49509 μM | SANGER | ||
| IGROV-1 | Growth Inhibition Assay | IC50=0.48797 μM | SANGER | ||
| RS4-11 | Growth Inhibition Assay | IC50=0.48584 μM | SANGER | ||
| BE-13 | Growth Inhibition Assay | IC50=0.48572 μM | SANGER | ||
| BHT-101 | Growth Inhibition Assay | IC50=0.4659 μM | SANGER | ||
| 697 | Growth Inhibition Assay | IC50=0.45633 μM | SANGER | ||
| NCI-H292 | Growth Inhibition Assay | IC50=0.44108 μM | SANGER | ||
| EM-2 | Growth Inhibition Assay | IC50=0.4389 μM | SANGER | ||
| H9 | Growth Inhibition Assay | IC50=0.43464 μM | SANGER | ||
| EoL-1-cell | Growth Inhibition Assay | IC50=0.41576 μM | SANGER | ||
| NCI-H209 | Growth Inhibition Assay | IC50=0.40808 μM | SANGER | ||
| DOK | Growth Inhibition Assay | IC50=0.37786 μM | SANGER | ||
| HCC1806 | Growth Inhibition Assay | IC50=0.35216 μM | SANGER | ||
| KU812 | Growth Inhibition Assay | IC50=0.34068 μM | SANGER | ||
| LAMA-84 | Growth Inhibition Assay | IC50=0.28664 μM | SANGER | ||
| HSC-4 | Growth Inhibition Assay | IC50=0.17158 μM | SANGER | ||
| CTV-1 | Growth Inhibition Assay | IC50=0.16398 μM | SANGER | ||
| SW756 | Growth Inhibition Assay | IC50=0.14024 μM | SANGER | ||
| NB7 | Growth Inhibition Assay | IC50=0.08231 μM | SANGER | ||
| SK-MEL-1 | Growth Inhibition Assay | IC50=4.18695 μM | SANGER | ||
| ABC-1 | Growth Inhibition Assay | IC50=4.23333 μM | SANGER | ||
| CAKI-1 | Growth Inhibition Assay | IC50=4.24571 μM | SANGER | ||
| HOS | Growth Inhibition Assay | IC50=4.29141 μM | SANGER | ||
| SN12C | Growth Inhibition Assay | IC50=4.34244 μM | SANGER | ||
| NB13 | Growth Inhibition Assay | IC50=4.37355 μM | SANGER | ||
| M14 | Growth Inhibition Assay | IC50=4.48792 μM | SANGER | ||
| GP5d | Growth Inhibition Assay | IC50=4.5012 μM | SANGER | ||
| NCI-H720 | Growth Inhibition Assay | IC50=4.53612 μM | SANGER | ||
| D-423MG | Growth Inhibition Assay | IC50=4.53924 μM | SANGER | ||
| ChaGo-K-1 | Growth Inhibition Assay | IC50=4.59559 μM | SANGER | ||
| MEL-HO | Growth Inhibition Assay | IC50=4.61261 μM | SANGER | ||
| MHH-ES-1 | Growth Inhibition Assay | IC50=4.62411 μM | SANGER | ||
| KYSE-270 | Growth Inhibition Assay | IC50=4.65126 μM | SANGER | ||
| GI-ME-N | Growth Inhibition Assay | IC50=4.71291 μM | SANGER | ||
| HOP-92 | Growth Inhibition Assay | IC50=4.81379 μM | SANGER | ||
| MKN1 | Growth Inhibition Assay | IC50=4.83914 μM | SANGER | ||
| ML-2 | Growth Inhibition Assay | IC50=4.85626 μM | SANGER | ||
| RO82-W-1 | Growth Inhibition Assay | IC50=4.9298 μM | SANGER | ||
| G-361 | Growth Inhibition Assay | IC50=5.01003 μM | SANGER | ||
| HC-1 | Growth Inhibition Assay | IC50=5.03291 μM | SANGER | ||
| EW-24 | Growth Inhibition Assay | IC50=5.04038 μM | SANGER | ||
| HuP-T4 | Growth Inhibition Assay | IC50=5.14334 μM | SANGER | ||
| 8-MG-BA | Growth Inhibition Assay | IC50=5.3428 μM | SANGER | ||
| HGC-27 | Growth Inhibition Assay | IC50=5.37682 μM | SANGER | ||
| TE-12 | Growth Inhibition Assay | IC50=5.41585 μM | SANGER | ||
| GT3TKB | Growth Inhibition Assay | IC50=5.44212 μM | SANGER | ||
| DOHH-2 | Growth Inhibition Assay | IC50=5.45986 μM | SANGER | ||
| Ca-Ski | Growth Inhibition Assay | IC50=5.46115 μM | SANGER | ||
| A172 | Growth Inhibition Assay | IC50=5.54925 μM | SANGER | ||
| EGI-1 | Growth Inhibition Assay | IC50=5.58938 μM | SANGER | ||
| MZ2-MEL | Growth Inhibition Assay | IC50=5.61486 μM | SANGER | ||
| SW1710 | Growth Inhibition Assay | IC50=5.69091 μM | SANGER | ||
| HT-144 | Growth Inhibition Assay | IC50=5.72685 μM | SANGER | ||
| PA-1 | Growth Inhibition Assay | IC50=5.81893 μM | SANGER | ||
| HCC1937 | Growth Inhibition Assay | IC50=5.83929 μM | SANGER | ||
| SK-OV-3 | Growth Inhibition Assay | IC50=5.91121 μM | SANGER | ||
| K5 | Growth Inhibition Assay | IC50=6.0517 μM | SANGER | ||
| NMC-G1 | Growth Inhibition Assay | IC50=6.07797 μM | SANGER | ||
| MDA-MB-361 | Growth Inhibition Assay | IC50=6.09261 μM | SANGER | ||
| EKVX | Growth Inhibition Assay | IC50=6.13501 μM | SANGER | ||
| ES7 | Growth Inhibition Assay | IC50=6.16115 μM | SANGER | ||
| KS-1 | Growth Inhibition Assay | IC50=6.17993 μM | SANGER | ||
| NCI-H661 | Growth Inhibition Assay | IC50=6.18081 μM | SANGER | ||
| ES8 | Growth Inhibition Assay | IC50=6.18082 μM | SANGER | ||
| NCI-H23 | Growth Inhibition Assay | IC50=6.21816 μM | SANGER | ||
| T47D | Growth Inhibition Assay | IC50=6.26457 μM | SANGER | ||
| A2780 | Growth Inhibition Assay | IC50=6.37701 μM | SANGER | ||
| SCC-4 | Growth Inhibition Assay | IC50=6.43561 μM | SANGER | ||
| VA-ES-BJ | Growth Inhibition Assay | IC50=6.97043 μM | SANGER | ||
| no-11 | Growth Inhibition Assay | IC50=7.1641 μM | SANGER | ||
| KU-19-19 | Growth Inhibition Assay | IC50=7.16476 μM | SANGER | ||
| MKN45 | Growth Inhibition Assay | IC50=7.18699 μM | SANGER | ||
| SCC-25 | Growth Inhibition Assay | IC50=7.23414 μM | SANGER | ||
| ETK-1 | Growth Inhibition Assay | IC50=7.25514 μM | SANGER | ||
| COR-L88 | Growth Inhibition Assay | IC50=7.29319 μM | SANGER | ||
| 8305C | Growth Inhibition Assay | IC50=7.32492 μM | SANGER | ||
| Detroit562 | Growth Inhibition Assay | IC50=7.32506 μM | SANGER | ||
| SNU-449 | Growth Inhibition Assay | IC50=7.37651 μM | SANGER | ||
| A704 | Growth Inhibition Assay | IC50=7.38278 μM | SANGER | ||
| D-502MG | Growth Inhibition Assay | IC50=7.38473 μM | SANGER | ||
| NCI-H2228 | Growth Inhibition Assay | IC50=7.41458 μM | SANGER | ||
| CHP-212 | Growth Inhibition Assay | IC50=7.51896 μM | SANGER | ||
| VMRC-RCZ | Growth Inhibition Assay | IC50=7.59066 μM | SANGER | ||
| RPMI-2650 | Growth Inhibition Assay | IC50=7.70312 μM | SANGER | ||
| HCC2218 | Growth Inhibition Assay | IC50=7.72258 μM | SANGER | ||
| GCT | Growth Inhibition Assay | IC50=7.82172 μM | SANGER | ||
| SW780 | Growth Inhibition Assay | IC50=7.9906 μM | SANGER | ||
| KMOE-2 | Growth Inhibition Assay | IC50=8.0407 μM | SANGER | ||
| KYSE-180 | Growth Inhibition Assay | IC50=8.08648 μM | SANGER | ||
| TE-1 | Growth Inhibition Assay | IC50=8.11057 μM | SANGER | ||
| OAW-42 | Growth Inhibition Assay | IC50=8.25496 μM | SANGER | ||
| VM-CUB-1 | Growth Inhibition Assay | IC50=8.28364 μM | SANGER | ||
| ECC10 | Growth Inhibition Assay | IC50=8.28397 μM | SANGER | ||
| SW1573 | Growth Inhibition Assay | IC50=8.44465 μM | SANGER | ||
| NCI-H1299 | Growth Inhibition Assay | IC50=8.59774 μM | SANGER | ||
| ALL-PO | Growth Inhibition Assay | IC50=8.66597 μM | SANGER | ||
| OVCAR-5 | Growth Inhibition Assay | IC50=8.77625 μM | SANGER | ||
| NCI-SNU-5 | Growth Inhibition Assay | IC50=8.83001 μM | SANGER | ||
| NCI-H2342 | Growth Inhibition Assay | IC50=8.83101 μM | SANGER | ||
| RPMI-7951 | Growth Inhibition Assay | IC50=8.84157 μM | SANGER | ||
| RCM-1 | Growth Inhibition Assay | IC50=9.08145 μM | SANGER | ||
| Daoy | Growth Inhibition Assay | IC50=9.12028 μM | SANGER | ||
| HCC1395 | Growth Inhibition Assay | IC50=9.30896 μM | SANGER | ||
| 786-0 | Growth Inhibition Assay | IC50=9.36026 μM | SANGER | ||
| GAMG | Growth Inhibition Assay | IC50=9.65534 μM | SANGER | ||
| HCC1954 | Growth Inhibition Assay | IC50=9.85859 μM | SANGER | ||
| NCI-H1838 | Growth Inhibition Assay | IC50=9.90371 μM | SANGER | ||
| SW620 | Growth Inhibition Assay | IC50=9.95357 μM | SANGER | ||
| NCI-H358 | Growth Inhibition Assay | IC50=10.4197 μM | SANGER | ||
| NCI-H1793 | Growth Inhibition Assay | IC50=10.4248 μM | SANGER | ||
| NCI-H1666 | Growth Inhibition Assay | IC50=10.4355 μM | SANGER | ||
| MZ7-mel | Growth Inhibition Assay | IC50=10.4753 μM | SANGER | ||
| MDA-MB-175-VII | Growth Inhibition Assay | IC50=10.6396 μM | SANGER | ||
| COLO-829 | Growth Inhibition Assay | IC50=10.8004 μM | SANGER | ||
| RVH-421 | Growth Inhibition Assay | IC50=11.152 μM | SANGER | ||
| A549 | Growth Inhibition Assay | IC50=11.2478 μM | SANGER | ||
| DJM-1 | Growth Inhibition Assay | IC50=11.3833 μM | SANGER | ||
| IST-MEL1 | Growth Inhibition Assay | IC50=11.7319 μM | SANGER | ||
| BEN | Growth Inhibition Assay | IC50=11.7402 μM | SANGER | ||
| KM12 | Growth Inhibition Assay | IC50=11.9091 μM | SANGER | ||
| HuO9 | Growth Inhibition Assay | IC50=12.0666 μM | SANGER | ||
| U-2-OS | Growth Inhibition Assay | IC50=12.0893 μM | SANGER | ||
| RH-1 | Growth Inhibition Assay | IC50=12.4472 μM | SANGER | ||
| NCI-H1048 | Growth Inhibition Assay | IC50=12.5506 μM | SANGER | ||
| Mo-T | Growth Inhibition Assay | IC50=12.7307 μM | SANGER | ||
| KYSE-150 | Growth Inhibition Assay | IC50=12.7455 μM | SANGER | ||
| A388 | Growth Inhibition Assay | IC50=12.7713 μM | SANGER | ||
| NCI-SNU-1 | Growth Inhibition Assay | IC50=12.8046 μM | SANGER | ||
| HEL | Growth Inhibition Assay | IC50=12.8212 μM | SANGER | ||
| UM-UC-3 | Growth Inhibition Assay | IC50=12.8874 μM | SANGER | ||
| TGBC24TKB | Growth Inhibition Assay | IC50=13.0267 μM | SANGER | ||
| SW626 | Growth Inhibition Assay | IC50=13.2485 μM | SANGER | ||
| ES6 | Growth Inhibition Assay | IC50=13.2512 μM | SANGER | ||
| NCI-H2029 | Growth Inhibition Assay | IC50=13.8108 μM | SANGER | ||
| RXF393 | Growth Inhibition Assay | IC50=13.9927 μM | SANGER | ||
| HMV-II | Growth Inhibition Assay | IC50=14.078 μM | SANGER | ||
| EW-22 | Growth Inhibition Assay | IC50=14.1502 μM | SANGER | ||
| AsPC-1 | Growth Inhibition Assay | IC50=14.564 μM | SANGER | ||
| COLO-678 | Growth Inhibition Assay | IC50=14.7271 μM | SANGER | ||
| HCT-15 | Growth Inhibition Assay | IC50=14.8855 μM | SANGER | ||
| HCE-T | Growth Inhibition Assay | IC50=14.8874 μM | SANGER | ||
| SF539 | Growth Inhibition Assay | IC50=15.0643 μM | SANGER | ||
| AU565 | Growth Inhibition Assay | IC50=15.2096 μM | SANGER | ||
| JVM-2 | Growth Inhibition Assay | IC50=15.2681 μM | SANGER | ||
| CaR-1 | Growth Inhibition Assay | IC50=15.4412 μM | SANGER | ||
| 23132-87 | Growth Inhibition Assay | IC50=15.8495 μM | SANGER | ||
| A673 | Growth Inhibition Assay | IC50=15.9636 μM | SANGER | ||
| KYSE-410 | Growth Inhibition Assay | IC50=16.029 μM | SANGER | ||
| TE-9 | Growth Inhibition Assay | IC50=16.062 μM | SANGER | ||
| LU-139 | Growth Inhibition Assay | IC50=16.1823 μM | SANGER | ||
| GCIY | Growth Inhibition Assay | IC50=16.1916 μM | SANGER | ||
| JEG-3 | Growth Inhibition Assay | IC50=16.25 μM | SANGER | ||
| RT-112 | Growth Inhibition Assay | IC50=16.4143 μM | SANGER | ||
| COLO-680N | Growth Inhibition Assay | IC50=16.5108 μM | SANGER | ||
| LU-134-A | Growth Inhibition Assay | IC50=16.9893 μM | SANGER | ||
| MFM-223 | Growth Inhibition Assay | IC50=17.1535 μM | SANGER | ||
| SF126 | Growth Inhibition Assay | IC50=17.1701 μM | SANGER | ||
| NCI-H28 | Growth Inhibition Assay | IC50=17.2066 μM | SANGER | ||
| BFTC-905 | Growth Inhibition Assay | IC50=17.4832 μM | SANGER | ||
| SCC-9 | Growth Inhibition Assay | IC50=17.6285 μM | SANGER | ||
| KNS-62 | Growth Inhibition Assay | IC50=17.6629 μM | SANGER | ||
| Hs-578-T | Growth Inhibition Assay | IC50=17.8149 μM | SANGER | ||
| D-336MG | Growth Inhibition Assay | IC50=17.8294 μM | SANGER | ||
| NCI-H82 | Growth Inhibition Assay | IC50=18.0183 μM | SANGER | ||
| EFM-19 | Growth Inhibition Assay | IC50=18.0577 μM | SANGER | ||
| TGBC11TKB | Growth Inhibition Assay | IC50=18.1021 μM | SANGER | ||
| HEC-1 | Growth Inhibition Assay | IC50=18.2918 μM | SANGER | ||
| HuP-T3 | Growth Inhibition Assay | IC50=18.5929 μM | SANGER | ||
| SF268 | Growth Inhibition Assay | IC50=18.6702 μM | SANGER | ||
| COLO-792 | Growth Inhibition Assay | IC50=18.7997 μM | SANGER | ||
| HLE | Growth Inhibition Assay | IC50=18.8331 μM | SANGER | ||
| A204 | Growth Inhibition Assay | IC50=18.9164 μM | SANGER | ||
| CAL-72 | Growth Inhibition Assay | IC50=19.0877 μM | SANGER | ||
| U031 | Growth Inhibition Assay | IC50=19.4909 μM | SANGER | ||
| FTC-133 | Growth Inhibition Assay | IC50=19.9304 μM | SANGER | ||
| SK-MEL-28 | Growth Inhibition Assay | IC50=20.3761 μM | SANGER | ||
| KGN | Growth Inhibition Assay | IC50=20.4699 μM | SANGER | ||
| HCC2998 | Growth Inhibition Assay | IC50=21.3926 μM | SANGER | ||
| GOTO | Growth Inhibition Assay | IC50=21.485 μM | SANGER | ||
| AGS | Growth Inhibition Assay | IC50=21.8451 μM | SANGER | ||
| EW-13 | Growth Inhibition Assay | IC50=22.1022 μM | SANGER | ||
| P12-ICHIKAWA | Growth Inhibition Assay | IC50=22.1603 μM | SANGER | ||
| NCI-H1395 | Growth Inhibition Assay | IC50=22.2907 μM | SANGER | ||
| A2058 | Growth Inhibition Assay | IC50=22.434 μM | SANGER | ||
| SH-4 | Growth Inhibition Assay | IC50=22.7045 μM | SANGER | ||
| DoTc2-4510 | Growth Inhibition Assay | IC50=23.6472 μM | SANGER | ||
| MMAC-SF | Growth Inhibition Assay | IC50=23.6911 μM | SANGER | ||
| NCI-H510A | Growth Inhibition Assay | IC50=23.7939 μM | SANGER | ||
| HDLM-2 | Growth Inhibition Assay | IC50=24.146 μM | SANGER | ||
| KINGS-1 | Growth Inhibition Assay | IC50=24.242 μM | SANGER | ||
| NCI-H1648 | Growth Inhibition Assay | IC50=24.4024 μM | SANGER | ||
| HCC1187 | Growth Inhibition Assay | IC50=25.0235 μM | SANGER | ||
| BALL-1 | Growth Inhibition Assay | IC50=25.2062 μM | SANGER | ||
| SBC-1 | Growth Inhibition Assay | IC50=25.2993 μM | SANGER | ||
| BFTC-909 | Growth Inhibition Assay | IC50=25.3551 μM | SANGER | ||
| MOLT-13 | Growth Inhibition Assay | IC50=25.6744 μM | SANGER | ||
| SW1990 | Growth Inhibition Assay | IC50=25.9655 μM | SANGER | ||
| DK-MG | Growth Inhibition Assay | IC50=26.0443 μM | SANGER | ||
| TE-8 | Growth Inhibition Assay | IC50=26.0668 μM | SANGER | ||
| Becker | Growth Inhibition Assay | IC50=26.1574 μM | SANGER | ||
| KYSE-70 | Growth Inhibition Assay | IC50=26.5317 μM | SANGER | ||
| MKN7 | Growth Inhibition Assay | IC50=27.7479 μM | SANGER | ||
| D-392MG | Growth Inhibition Assay | IC50=27.7694 μM | SANGER | ||
| NH-12 | Growth Inhibition Assay | IC50=28.1229 μM | SANGER | ||
| EW-18 | Growth Inhibition Assay | IC50=28.2218 μM | SANGER | ||
| LCLC-97TM1 | Growth Inhibition Assay | IC50=28.2762 μM | SANGER | ||
| NCI-H1770 | Growth Inhibition Assay | IC50=28.3566 μM | SANGER | ||
| BT-20 | Growth Inhibition Assay | IC50=28.3685 μM | SANGER | ||
| DBTRG-05MG | Growth Inhibition Assay | IC50=28.4838 μM | SANGER | ||
| HPAF-II | Growth Inhibition Assay | IC50=28.779 μM | SANGER | ||
| SW837 | Growth Inhibition Assay | IC50=29.3385 μM | SANGER | ||
| 647-V | Growth Inhibition Assay | IC50=29.7003 μM | SANGER | ||
| J82 | Growth Inhibition Assay | IC50=29.8013 μM | SANGER | ||
| MC116 | Growth Inhibition Assay | IC50=30.0733 μM | SANGER | ||
| NCI-H69 | Growth Inhibition Assay | IC50=30.6093 μM | SANGER | ||
| NB6 | Growth Inhibition Assay | IC50=31.3629 μM | SANGER | ||
| CAL-120 | Growth Inhibition Assay | IC50=32.4317 μM | SANGER | ||
| U-87-MG | Growth Inhibition Assay | IC50=33.0251 μM | SANGER | ||
| NCI-H1304 | Growth Inhibition Assay | IC50=33.0354 μM | SANGER | ||
| YH-13 | Growth Inhibition Assay | IC50=33.2535 μM | SANGER | ||
| RMG-I | Growth Inhibition Assay | IC50=33.4285 μM | SANGER | ||
| LU-65 | Growth Inhibition Assay | IC50=34.1408 μM | SANGER | ||
| GB-1 | Growth Inhibition Assay | IC50=35.0729 μM | SANGER | ||
| DU-4475 | Growth Inhibition Assay | IC50=35.1553 μM | SANGER | ||
| SBC-5 | Growth Inhibition Assay | IC50=36.5902 μM | SANGER | ||
| OE33 | Growth Inhibition Assay | IC50=37.7577 μM | SANGER | ||
| C8166 | Growth Inhibition Assay | IC50=38.5267 μM | SANGER | ||
| COLO-684 | Growth Inhibition Assay | IC50=38.7428 μM | SANGER | ||
| NCI-H1155 | Growth Inhibition Assay | IC50=39.0471 μM | SANGER | ||
| ATN-1 | Growth Inhibition Assay | IC50=39.7792 μM | SANGER | ||
| KARPAS-299 | Growth Inhibition Assay | IC50=39.839 μM | SANGER | ||
| KNS-81-FD | Growth Inhibition Assay | IC50=40.3604 μM | SANGER | ||
| NCI-H1563 | Growth Inhibition Assay | IC50=41.5039 μM | SANGER | ||
| NB14 | Growth Inhibition Assay | IC50=42.7263 μM | SANGER | ||
| COLO-800 | Growth Inhibition Assay | IC50=42.8517 μM | SANGER | ||
| MS-1 | Growth Inhibition Assay | IC50=43.0483 μM | SANGER | ||
| OVCAR-8 | Growth Inhibition Assay | IC50=43.6809 μM | SANGER | ||
| SK-PN-DW | Growth Inhibition Assay | IC50=43.8776 μM | SANGER | ||
| G-402 | Growth Inhibition Assay | IC50=43.9006 μM | SANGER | ||
| NCI-H2291 | Growth Inhibition Assay | IC50=44.8017 μM | SANGER | ||
| PC-3 | Growth Inhibition Assay | IC50=45.8023 μM | SANGER | ||
| NCI-H1581 | Growth Inhibition Assay | IC50=45.9889 μM | SANGER | ||
| SW1116 | Growth Inhibition Assay | IC50=47.0182 μM | SANGER | ||
| ZR-75-30 | Growth Inhibition Assay | IC50=47.0239 μM | SANGER | ||
| OCI-AML2 | Growth Inhibition Assay | IC50=47.0918 μM | SANGER | ||
| MDA-MB-231 | Growth Inhibition Assay | IC50=47.6249 μM | SANGER | ||
| ES3 | Growth Inhibition Assay | IC50=48.3529 μM | SANGER | ||
| NCI-H630 | Growth Inhibition Assay | IC50=49.1742 μM | SANGER | ||
| OE19 | Growth Inhibition Assay | IC50=49.2902 μM | SANGER | ||
| NCI-H1573 | Growth Inhibition Assay | IC50=49.6861 μM | SANGER | ||
| EW-1 | Growth Inhibition Assay | IC50=49.9084 μM | SANGER | ||
| fibroblast cells | Antiproliferative assay | Antiproliferative activity against Src-transformed rat2 fibroblast cells, IC50 = 0.1 μM. | 17181170 | ||
| fibroblast cells | Function assay | Inhibition of human cSrc-vSrc fusion protein expressed in rat fibroblast cells by ELISA, IC50 = 0.1 μM. | 17905586 | ||
| Ba/F3 | Function assay | Inhibition of NPM/ALK L256T mutant kinase activity in BaF3 cells by radioenzymatic assay, IC50 = 0.15 μM. | 16970400 | ||
| Ba/F3 | Antiproliferative assay | Antiproliferative activity against murine BaF3 cells expressing NPM/ALK L256T mutant by [3H]thymidine uptake assay, IC50 = 0.2 μM. | 16970400 | ||
| Ba/F3 | Function assay | Inhibition of NPM/ALK L256T mutant autophosphorylation activity in BaF3 cells by antiphosphotyrosine immunoblotting assay, IC50 = 0.2 μM. | 16970400 | ||
| fibroblast cells | Function assay | Inhibitory concentration against Abl transformed rat fibroblast cells, IC50 = 0.49 μM. | 16161995 | ||
| Ba/F3 | Antiproliferative assay | Antiproliferative activity against murine BaF3 cells expressing wild type NPM/ALK by [3H]thymidine uptake assay, IC50 = 1 μM. | 16970400 | ||
| Ba/F3 | Cell death assay | Induction of cell death of murine BaF3 cells expressing NPM/ALK L256T mutant by trypan blue exclusion assay | 16970400 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 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(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Bosutinib是一種新型的雙重Src/Abl抑制劑，在無細(xì)胞試驗(yàn)中IC50分別為1.2 nM 和 1 nM。Bosutinib也可通過阻滯p-ERK、p-S6和p-STAT3的磷酸化來有效地降低PI3K/AKT/mTOR、MAPK/ERK和JAK/STAT3信號通路的活性。Bosutinib可促進(jìn)自噬。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶點(diǎn) |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | Bosutinib作用于Src比非Src家族激酶選擇性高，IC50為1.2 nM,且有效抑制Src依賴的細(xì)胞增殖，IC50為100 nM。[1] Bosutinib 顯著抑制Bcr-Abl陽性白血病細(xì)胞系KU812, K562, 和MEG-01 而不是 Molt-4, HL-60, Ramos, 和其他白血病細(xì)胞系的增殖，IC50分別為5 nM, 20 nM,和20 nM，比 STI-571更有效。與STI-571類似, Bosutinib 作用于Abl-MLV轉(zhuǎn)化纖維，具有看增殖活性，IC50為 90 nM。Bosutinib濃度分別為50 nM, 10-25 nM, 和200 nM 時(shí),切除CML細(xì)胞中的Bcr-Abl 和STAT5及纖維中表達(dá)的v-Abl酪氨酸磷酸化，導(dǎo)致Bcr-Abl下游信號Lyn/Hck 磷酸化受抑制。[2] 雖然不能抑制乳腺癌細(xì)胞增殖和存活，但是可明顯降低乳腺癌細(xì)胞運(yùn)動和入侵，IC50為250 nM,提高細(xì)胞間粘附和β-連環(huán)蛋白的膜定位。[3] |
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|---|---|---|---|---|
| 激酶實(shí)驗(yàn) | Src和Abl激酶實(shí)驗(yàn) | |||
| 使用ELISA法測定Src激酶活性。Src(每次反應(yīng)3單位), 反應(yīng)buffer(50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.5 mM Na3VO4)和cdc2底物肽，加入不同濃度Bosutinib，然后在30oC下溫育10分鐘。加入ATP，終濃度為 100 μM,開始反應(yīng)，30oC下溫育1小時(shí)，然后加入 EDTA終止反應(yīng)。在DELFIA 固相基于銪的檢測法格板上進(jìn)行 Abl 激酶實(shí)驗(yàn)。2 μM生物素化的肽段結(jié)合到鏈霉親和素包被的微量滴定板上，在溶于PBS的1 mg/mL 卵清蛋白中進(jìn)行1.5小時(shí)。用PBS/0.1% Tween-80沖洗板1小時(shí)，隨后用PBS 沖洗。激酶反應(yīng)在30oC下進(jìn)行1小時(shí)。Abl激酶(10單位)與50 mM Tris-HCl(pH 7.5),10 mM MgCl2, 80 μM EGTA, 100 μM ATP, 0.5 mM Na3VO4,1% DMSO,1 mM HEPES (pH 7.0),200 μg/mL 卵清蛋白及不同濃度 Bosutinib混合。加入EDTA反應(yīng)終止，終濃度為50 mM。使用Eu標(biāo)記的磷酸酪氨酸抗體和DELFIA增強(qiáng)液監(jiān)測反應(yīng)。 | ||||
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | Abl-MLV,Rat 2,KU812,K562,和MEG-01 | ||
| 濃度 | 溶于DMSO,終濃度為1 μM 左右 | |||
| 孵育時(shí)間 | 72小時(shí) | |||
| 方法 | 用不同濃度Bosutinib處理細(xì)胞72小時(shí)。在Sigmacote處理的超低結(jié)合96孔板上檢測Abl-MLV轉(zhuǎn)化纖維的Anchorage非依賴增殖，阻止剩余細(xì)胞粘附。使用MTS或 Cell-Glo測定細(xì)胞增殖。為了測定細(xì)胞周期或者細(xì)胞死亡，細(xì)胞準(zhǔn)備在CycleTest和DNA試劑盒中，用于FACS分析，在熒光激活的細(xì)胞分選流式細(xì)胞儀中進(jìn)行分析。 |
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| 實(shí)驗(yàn)圖片 | 檢測方法 | 檢測指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | p-ABL / ABL p-FAK / FAK / p-Pyk2 / p-p130Cas / p-AKT p-Src / Src / p-c-Abl / c-Abl / p-S6 / S6 / p-ERK / ERK / p-STAT3 / STAT3 |
|
28199182 | |
| Immunofluorescence | p-FAK / p-STAT3 / beta-catenin |
|
18483306 | |
| Growth inhibition assay | IC50 Cell viability |
|
27903968 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | Bosutinib每天按60 mg/kg劑量有效作用于攜帶Src-轉(zhuǎn)化纖維移植瘤和HT29移植瘤的裸鼠，T/C值分別為18%和30%。[1] Bosutinib口服給藥小鼠5天，顯著抑制K562 腫瘤生長，這種作用存在劑量依賴性，按100 mg/kg 劑量處理可根除大的腫瘤，按150 mg/kg劑量處理可除去腫瘤，且沒有毒性。[2] 與作用于HT29 移植瘤的效果相比，Bosutinib按 75 mg/kg劑量作用于攜帶Colo205移植瘤的裸鼠，每天兩次，可抑制腫瘤生長，提高劑量后不會有更高效果，但是 按50 mg/kg劑量處理則沒有效果。[4] |
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|---|---|---|
| 動物實(shí)驗(yàn) | Animal Models | 注射K562細(xì)胞的雌性裸鼠 |
| Dosages | 150 mg/kg/day | |
| Administration | 口服飼喂 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05363488 | Completed | Myeloid Leukemia |
Pfizer |
October 8 2021 | -- |
| NCT04258943 | Active not recruiting | Philadelphia Chromosome Positive CML|Accelerated Phase Chronic Myelogenous Leukemia|Blastic Phase Chronic Myelogenous Leukemia|Chronic Phase Chronic Myelogenous Leukemia |
Children''s Oncology Group|Erasmus Medical Center|Dutch Childhood Oncology Group|Innovative Therapies for Children with Cancer|Pfizer |
April 6 2020 | Phase 1|Phase 2 |
| NCT03023319 | Completed | Carcinoma Non-Small-Cell Lung|Mesothelioma|Bladder Cancer|Ovarian Cancer|Peritoneal Cancer|Thymoma|Thymus Cancer|Uterine Cervical Cancer |
Nagla Abdel Karim|Augusta University |
December 10 2019 | Phase 1 |
| NCT03888222 | Completed | Dementia With Lewy Bodies |
Georgetown University|Alzheimer''s Association |
April 23 2019 | Phase 2 |
| NCT03854903 | Active not recruiting | Metastatic Breast Cancer|Human Epidermal Growth Factor 2 Negative Carcinoma of Breast|Hormone Receptor Positive Breast Cancer |
Georgetown University|Pfizer |
April 1 2019 | Phase 1 |
化學(xué)信息&溶解度
| 分子量 | 530.45 | 分子式 | C26H29Cl2N5O3 |
| CAS號 | 380843-75-4 | SDF | Download Bosutinib SDF |
| Smiles | CN1CCN(CC1)CCCOC2=C(C=C3C(=C2)N=CC(=C3NC4=CC(=C(C=C4Cl)Cl)OC)C#N)OC | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 100 mg/mL ( (188.51 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(jì)算器 |
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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(jì)算器 | ||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)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(jì)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(jìn)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:
Can I give S1014 Bosutinib to mice by oral gavage? If so, how to dissolve the drug?
回答：
For oral gavage, S1014 Bosutinib can be dissolved in 5% Tween 80+0.5% CMC Na at 30 mg/ml as a suspension.
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