BPI-9016M是一种有效的，口服活性的，选择性的双重 c-Met 和 AXL 酪氨酸激酶抑制剂。BPI-9016M抑制肺腺癌的肿瘤细胞生长，迁移和侵袭。
| Cas No. | 1528546-94-2 |
| 分子式 | C25H18F2N4O3 |
| 分子量 | 460.43 |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | BPI-9016M is a potent, orally active, and selective dualc-MetandAXLtyrosine kinases inhibitor. BPI-9016M suppresses tumor cell growth, migration and invasion of lung adenocarcinoma[1][2]. BPI-9016M (6.3-25 μM; 2 weeks) inhibited cell proliferation[2].
BPI-9016M (12.5-50 μM; 24 hpurs) induces accumulation of more tumor cells in the G1 phase[2].
BPI-9016M (3.1-50 μM) reduces expression of c-Met, p-c-Met, p-AKT and p-ERK in the H1299 and A549 cells in a dose-dependent manner[2].
The IC50of BPI-9016M in several lung adenocarcinoma cell lines ( A549, H1299, H1650, H1975, HCC827, and PC-9 cells) as well as in primary lung adenocarcinoma cells are ranged from 5.3 μM to 27.1 μM[2]. Cell Proliferation Assay[2] | Cell Line: | A549 and H1299 cells | | Concentration: | 6.3, 12.5, 25 μM | | Incubation Time: | 2 weeks | | Result: | Colony formation was significantly inhibited in a dose-dependent manner. |
Cell Cycle Analysis[2] | Cell Line: | A549 and H1299 cells | | Concentration: | 12.5, 25, 50 μM | | Incubation Time: | 24 hours | | Result: | Induced accumulation of more tumor cells in the G1 phase. |
BPI-9016M (60 mg/kg; p.o.; daily for 16 or 12 days) dramatically restrains tumor growth in PDX xenografts in NOD/SCID mice[2]. | Animal Model: | NOD/SCID mice[2] | | Dosage: | 60 mg/kg | | Administration: | p.o.; daily for 16 or 12 days | | Result: | Dramatically restrained tumor growth in PDX xenografts in NOD/SCID mice. |
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