Antibodies
BMS-794833
- 貨號 Cat. No.
- S2201
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
BMS-794833
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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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
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 | VEGFR2 | ||||
| IC50 | 1.7 nM | 15 nM [1] | ||||
| 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] | |||||
| Features | ||||||
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% glycerol). The reaction is initiated by addition of enzyme and stopped by 30% TCA after 1 hour. Assays are prepared in 96 well plates and incubated at 27 °C for 1 hour. Then acid precipitated with TCA for 20 minutes on ice. Those precipitates are transferred to GF/C plates using a 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. |
Animal Study: [1]
| Animal Models | GTL-16 and U87 xenografts |
|---|---|
| Dosages | 25 mg/kg |
| Administration | Orally once daily |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00792558 | Withdrawn | Advanced Solid Tumors | Bristol-Myers Squibb | 2009-01 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 468.84 |
|---|---|
| Formula | C23H15ClF2N4O3 |
| CAS No. | 1174046-72-0 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 94 mg/mL (200 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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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.46884 | 4.6884 | 9.3768 | 14.0652 |
