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BMS-794833

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Catalog No. T2419Cas No. 1174046-72-0

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

BMS-794833

BMS-794833

🥰Excellent
Purity: 99.69%
Catalog No. T2419Cas No. 1174046-72-0
BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2; a prodrug of BMS-817378.
Pack SizePriceAvailabilityQuantity
1 mg$35In Stock
2 mg$48In Stock
5 mg$90In Stock
10 mg$153In Stock
25 mg$312In Stock
50 mg$566In Stock
100 mg$812In Stock
1 mL x 10 mM (in DMSO)$96In Stock
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Purity:99.69%
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Product Introduction

Bioactivity
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)
Chemical Properties
Molecular Weight468.84
FormulaC23H15ClF2N4O3
Cas No.1174046-72-0
SmilesNc1nccc(Oc2ccc(NC(=O)c3c[nH]cc(-c4ccc(F)cc4)c3=O)cc2F)c1Cl
Relative Density.1.508 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
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)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.1329 mL10.6646 mL21.3292 mL106.6462 mL
5 mM0.4266 mL2.1329 mL4.2658 mL21.3292 mL
10 mM0.2133 mL1.0665 mL2.1329 mL10.6646 mL
20 mM0.1066 mL0.5332 mL1.0665 mL5.3323 mL
50 mM0.0427 mL0.2133 mL0.4266 mL2.1329 mL
100 mM0.0213 mL0.1066 mL0.2133 mL1.0665 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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