For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I017232 |
| CAS Number | 1528546-94-2 |
| Synonyms | N-[4-(2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-4-yloxy)-3-fluorophenyl]-5-(4-fluorophenyl)-4-oxo-1H-pyridine-3-carboxamide |
| Molecular Formula | C25H18F2N4O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H18F2N4O3/c26-15-3-1-14(2-4-15)18-12-28-13-19(23(18)32)25(33)31-16-5-6-22(20(27)11-16)34-21-8-10-30-24-17(21)7-9-29-24/h1-6,8,10-13H,7,9H2,(H,28,32)(H,29,30)(H,31,33) |
| InChIKey | DGMFNZXEGKFREH-UHFFFAOYSA-N |
| SMILES | C1CNC2=NC=CC(=C21)OC3=C(C=C(C=C3)NC(=O)C4=CNC=C(C4=O)C5=CC=C(C=C5)F)F |
| Reference | [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. |
