Home Protein Tyrosine Kinase c-Met inhibitor - VEGFR inhibitor - RON inhibitor BMS-794833 For research use only.

BMS-794833

BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1.

BMS-794833 Chemical Structure

BMS-794833 Chemical Structure

CAS No. 1174046-72-0

Purity & Quality Control

BMS-794833 Related Products

Signaling Pathway

c-Met Signaling Pathways

c-Met Signaling Pathway

Biological Activity

Description BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1.
Targets
Met [1] VEGFR2 [1]
1.7 nM 15 nM
In vitro
In vitro BMS794833 also inhibits Met receptor activated gastric carcinoma cell line, GTL-16, with IC50 of 39 nM. [1]
Kinase Assay Met kinase assay
BMS798433 is dissolved in DMSO and diluted by water before use. The reaction solution contains baculovirus expressed GST-Met kinase, 20 mM Tris-HCl (pH 7.4), 1 mM MnCl2, 1 mM DTT, 0.1mg BSA, 0.1 mg polyGlu4/tyr, 1µM ATP and 0.2µCi γ–ATP. Reactions are incubated at 30 °C for 1 hour and stopped by 8% TCA. TCA precipitates are collected onto GF/C plates using a universal harvester and the filters are quantitated using liquid scintillation counter.
Cell Research Cell lines GTL-16 cells
Concentrations ~ 1 μM
Incubation Time 72 hours
Method GTL-16 cells are seeded into 96 well plates and incubated for 24 hours. BMS798433 is dissolved in DMSO at 10 mM and diluted with culture medium before use. Then BMS798433 is added to the cells for 72 hours. After that, MTS assay is used to measure the IC50.
In Vivo
In vivo In GTL-16 human gastric tumor xenografts model, BMS798433 shows greater than 50% TGI for at least one tumor doubling time with no overt toxicity observed during 14 days. BMS798433 also shows complete tumor stasis at a dose of 25 mg/kg against U87 glioblastoma model. [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00792558 Withdrawn
Advanced Solid Tumors
Bristol-Myers Squibb
 January 2009 Phase 1

Chemical Information & Solubility

Molecular Weight 468.84 Formula

C23H15ClF2N4O3
CAS No. 1174046-72-0 SDF Download BMS-794833 SDF
Smiles C1=CC(=CC=C1C2=CNC=C(C2=O)C(=O)NC3=CC(=C(C=C3)OC4=C(C(=NC=C4)N)Cl)F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 94 mg/mL ( (200.49 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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