BMS-794833

Catalog No.S2201 Batch:S220101

Technical Data

Formula	C₂₃H₁₅ClF₂N₄O₃
Molecular Weight	468.84	CAS No.	1174046-72-0
Solubility (25°C)*	In vitro	DMSO	94 mg/mL (200.49 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 (from 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.
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.

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.

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.

References

[1] WO2009094417A1

Selleck's BMS-794833 has been cited by 1 publication

Polypharmacological reprogramming of tumor-associated macrophages towards an inflammatory phenotype [ Cancer Res, 2021, canres.1428.2021]	PubMed: 34903600

Polypharmacological reprogramming of tumor-associated macrophages towards an inflammatory phenotype [ Cancer Res, 2021, canres.1428.2021]

PubMed: 34903600

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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