4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
产品详情
BPI-9016M是一种有效的,口服活性的,选择性的双重 c-Met 和 AXL 酪氨酸激酶抑制剂。BPI-9016M抑制肺腺癌的肿瘤细胞生长,迁移和侵袭。
生物活性
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.
性状
Solid
体外研究(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 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: NOD/SCID mi
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (217.19 mM; Need ultrasonic)配制储备液