| Description |
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].
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| Related Catalog |
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| In Vitro |
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.
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| 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[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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| References |
[1]. Zhang P, et al. BPI-9016M, a c-Met inhibitor, suppresses tumor cell growth, migration and invasion of lung adenocarcinoma via miR203-DKK1. Theranostics. 2018 Nov 12;8(21):5890-5902. [2]. Hu X, et al. First-in-human phase I study of BPI-9016M, a dual MET/Axl inhibitor, in patients with non-small cell lung cancer.J Hematol Oncol. 2020 Jan 16;13(1):6.
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