product name BMS-794833
Description: BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7 nM/15 nM. BMS-794833 also inhibits Ron (Met family), Axl and Flt-3 with IC50 values less than 3 nM. It is selective versus a panel of greater than 200 additional receptor tyrosine kinase (RTKs), non-RTKs and serine/threonine kinases based on biochemical or Ambit binding assays. In vivo, BMS-794833 exhibited dose-dependent anti-tumor activity against multiple tumor types without overt toxicities at efficacious dose levels.
References: WO2009094417A1
468.84
Formula
C23H15ClF2N4O3
CAS No.
1174046-72-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 94 mg/mL (200.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19402740
| In Vitro |
In vitro activity: BMS794833 also inhibits Met receptor activated gastric carcinoma cell line, GTL-16, with IC50 of 39 nM. 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: 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. |
|---|---|
| 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. |
| Animal model | human gastric tumor xenografts model and U87 glioblastoma model |
| Formulation & Dosage | 25mg/kg |
| References |
Related Posts
product name BMS-794833
Description: BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7 nM/15 nM. BMS-794833 also inhibits Ron (Met family), Axl and Flt-3 with IC50 values less than 3 nM. It is selective versus a panel of greater than 200 additional receptor tyrosine kinase (RTKs), non-RTKs and serine/threonine kinases based on biochemical or Ambit binding assays. In vivo, BMS-794833 exhibited dose-dependent anti-tumor activity against multiple tumor types without overt toxicities at efficacious dose levels.
References: WO2009094417A1
468.84
Formula
C23H15ClF2N4O3
CAS No.
1174046-72-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 94 mg/mL (200.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19402740
| In Vitro |
In vitro activity: BMS794833 also inhibits Met receptor activated gastric carcinoma cell line, GTL-16, with IC50 of 39 nM. 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: 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. |
|---|---|
| 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. |
| Animal model | human gastric tumor xenografts model and U87 glioblastoma model |
| Formulation & Dosage | 25mg/kg |
| References |