Catalog No.S2201

BMS-794833 is a potent ATP competitive inhibitor of 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.

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BMS-794833 Chemical Structure

BMS-794833 Chemical Structure
Molecular Weight: 468.84

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Product Information

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Product Description

Biological Activity

Description BMS-794833 is a potent ATP competitive inhibitor of 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]
IC50 1.7 nM 15 nM
In vitro BMS794833 also inhibits Met receptor activated gastric carcinoma cell line, GTL-16, with IC50 of 39 nM. [1]
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]

Protocol(Only for Reference)

Kinase Assay: [1]

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.
VEGFR2 assay BMS798433 is dissolved in DMSO and diluted by water before use. The reaction solution contains 20 mM Tris-HCl (pH 7.4), 1 mM MnCl2, 1 mM DTT, 0.1mg BSA, 75 µg polyGlu4/tyr, 1µM ATP, 0.5 µCi γ–ATP and 7.5 ng/rxn enzyme stock (10% glyc

Cell Assay: [1]

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.

Animal Study: [1]

Animal Models GTL-16 and U87 xenografts
Dosages 25 mg/kg
Administration Orally once daily

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] WO2009094417A1

Chemical Information

Download BMS-794833 SDF
Molecular Weight (MW) 468.84


CAS No. 1174046-72-0
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 94 mg/mL (200.49 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-5-(4-fluorophenyl)-4-oxo-1,4-dihydropyridine-3-carboxamide

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