BPI-9016M is an effective, orally active, and selective dual inhibitor of c-Met and AXL tyrosine kinases. It suppresses tumor cell growth, invasion, and migration of lung adenocarcinoma.

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. BPI-9016M (3.1-50 μM) reduces the expression of c-Met, p-c-Met, p-AKT, and p-ERK in the H1299 and A549 cells in a dose-dependent manner. BPI-9016M (6.3-25 μM; 2 weeks) inhibited cell proliferation. BPI-9016M (12.5-50 μM; 24 hours) induces the accumulation of more tumor cells in the G1 phase [2].

In PDX xenografts in NOD/SCID mice, BPI-9016M (60 mg/kg; p.o.; daily for 16 or 12 days) dramatically restrains tumor growth [2].

1528546-94-2

C25H18F2N4O3

460.43

BPI-9016M

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years