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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

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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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$32In StockIn Stock
5 mg$73In StockIn Stock
10 mg$123In StockIn Stock
25 mg$198In StockIn Stock
50 mg$372In StockIn Stock
100 mg$619In StockIn Stock
1 mL x 10 mM (in DMSO)$75In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.69%
Color:White
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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
VEGFR2:15 nM, MET:1.7 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/Shipping at ambient temperature.
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 117.5 mg/mL (250.62 mM), Sonication is recommended.
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.04 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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