| CAS NO: | 1174046-72-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 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 | |
| SMILES | O=C(C1=CNC=C(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=C(Cl)C(N)=NC=C4)C(F)=C3 |
| Synonyms | BMS-794833; BMS 794833; BMS794833; N-(4-((2-amino-3-chloropyridin-4-yl)oxy)-3-fluorophenyl)-5-(4-fluorophenyl)-4-oxo-1,4-dihydropyridine-3-carboxamide InChi Key: PDYXPCKITKHFOZ-UHFFFAOYSA-N InChi Code: InChI=1S/C23H15ClF2N4O3/c24-20-19(7-8-29-22(20)27)33-18-6-5-14(9-17(18)26)30-23(32)16-11-28-10-15(21(16)31)12-1-3-13(25)4-2-12/h1-11H,(H2,27,29)(H,28,31)(H,30,32) SMILES Code: O=C(C1=CNC=C(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=C(Cl)C(N)=NC=C4)C(F)=C3 |
| 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 | WO2009094417 |
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