BPI-9016M is a potent, orally active, and selective dual c-Met and AXL tyrosine 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 IC50 of 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. |