BPI-9016M

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. In Vitro BPI-9016M (6.3-25 μM; 2 weeks) inhibited cell proliferation. BPI-9016M (12.5-50 μM; 24 hpurs) induces accumulation of more tumor cells in the G1 phase. 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. The IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell 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 AnalysisCell 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. In Vivo BPI-9016M (60 mg/kg; p.o.; daily for 16 or 12 days) dramatically restrains tumor growth in PDX xenografts in NOD/SCID mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NOD/SCID miceDosage: 60 mg/kg Administration: p.o.; daily for 16 or 12 days Result: Dramatically restrained tumor growth in PDX xenografts in NOD/SCID mice. Form:Solid

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