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
Especificações
Especificações e pureza
≥97%
Mecanismos bioquímicos e fisiológicos
BPI-9016M is a potent, orally active, andxa0selective dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses tumor cell growth, migration and invasion of lung adenocarcinoma.
Condições de armazenamento de armazenamento
Store at 2-8°C,Protected from light,Desiccated
Enviado em
Wet ice
Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.
Tipo de ação
INHIBITOR
Pureza
≥97%
Nomes e identificadores
Peso molecular
460.43
Dados avançados
Certificados(CoA,COO,BSE/TSE e Mapa de Análise)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Propriedades químicas e físicas
Solubilidade
DMSO : 100 mg/mL (217.19 mM; Need ultrasonic)
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