1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR
  3. BPI-9016M

BPI-9016M 

Cat. No.: HY-114356
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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.

For research use only. We do not sell to patients.

BPI-9016M Chemical Structure

BPI-9016M Chemical Structure

CAS No. : 1528546-94-2

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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].

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.
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.
Clinical Trial
Molecular Weight

460.43

Formula

C₂₅H₁₈F₂N₄O₃

CAS No.

1528546-94-2

SMILES

O=C(C1=CNC=C(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=C5C(NCC5)=NC=C4)C(F)=C3

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

BPI-9016Mc-Met/HGFRtomorcellgrowthmigrationinvasionlungadenocarcinoma,proliferationNOD/SCIDmiceInhibitorinhibitorinhibit

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