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BMS-794833

Catalog No. T2419   CAS 1174046-72-0

BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2; a prodrug of BMS-817378.

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BMS-794833 Chemical Structure
BMS-794833, CAS 1174046-72-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 35.00
2 mg In stock $ 48.00
5 mg In stock $ 90.00
10 mg In stock $ 153.00
25 mg In stock $ 312.00
50 mg In stock $ 566.00
100 mg In stock $ 812.00
1 mL * 10 mM (in DMSO) In stock $ 96.00
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Purity: 99.79%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2; a prodrug of BMS-817378.
Targets&IC50 MET:1.7 nM, VEGFR2:15 nM
In vitro At a dosage of 25 mg/kg, BMS798433 exhibited complete inhibition of tumor growth in the U87 glioblastoma model. In the GTL-16 human gastric tumor xenograft model, treatment with BMS798433 for 14 days resulted in a Tumor Growth Inhibition (TGI) rate of over 50% within at least one tumor doubling time, with no significant toxicity observed during the period.
In vivo BMS794833 inhibits the activation of the Met receptor in the gastric cancer cell line GTL-16, with an IC50 of 39 nM.
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, 0.1 mg BSA, 0.1 mg polyGlu4/tyr, 1 μM 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 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.(Only for Reference)
Molecular Weight 468.84
Formula C23H15ClF2N4O3
CAS No. 1174046-72-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 87 mg/mL (185.6 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. WO2009094417A1

Related compound libraries

This product is contained In the following compound libraries:
Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Inhibitor Library Anti-Breast Cancer Compound Library ReFRAME Related Library Cytokine Inhibitor Library Anti-Lung Cancer Compound Library Preclinical Compound Library Reprogramming Compound Library

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Keywords

BMS-794833 1174046-72-0 Angiogenesis Tyrosine Kinase/Adaptors VEGFR c-Met/HGFR BMS794833 Inhibitor inhibit Vascular endothelial growth factor receptor BMS 794833 inhibitor

 

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