PHA-665752 hydrate
- английское имя(2R)-1-[[5-[(Z)-[5-[[(2,6-DICHLOROPHENYL)METHYL]SULFONYL]-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE]METHYL]-2,4-DIMETHYL-1H-PYRROL-3-YL]CARBONYL]-2-(1-PYRROLIDINYLMETHYL)PYRROLIDINE
- CAS №477575-56-7
- CBNumberCB72448634
- ФормулаC32H34Cl2N4O4S
- мольный вес641.61
- номер MDLMFCD07772270
- файл Mol477575-56-7.mol
химическое свойство
Температура кипения | 890.2±65.0 °C(Predicted) |
плотность | 1.404 |
температура хранения | Sealed in dry,2-8°C |
растворимость | DMSO: ≥20mg/mL |
форма | powder |
пка | 11.39±0.20(Predicted) |
цвет | light yellow to light brown |
оптическая активность | [α]/D +50 to +70°, c = 0.2 in methanol |
FDA UNII | 0VXU5T5R3J |
PHA-665752 hydrate химические свойства, назначение, производство
Описание
The c-Химические свойства
Yellow powder crystalИспользование
PHA-665752 ia a c-Met kinase inhibitor. PHA-665752 is ATP-competitive, an active-site inhibitor with greater than 50-fold selectivity for c-Met vs a panel of tyrosine and serine-threonine kinases.Определение
ChEBI: A member of the class of indolones that is 1,3-dihydro-2H-indol-2-one which is substituted by a (2,6-dichlorobenzyl)sulfonyl group at position 5 and by a (1H-pyrrol-2-yl)methylidene group at position 2, the pyrrole rin of which is substituted by methyl groups at positions 3 and 5, and by a [2-(pyrrolidin-1-ylmethyl)pyrrolidin-1-yl]carbonyl group at position 4 (the Z,R isomer).Биологическая активность
Potent, selective and ATP-competitive inhibitor of MET kinase (IC 50 values are 9, 68, 200, 1400, 3000, 3800 and 6000 nM for MET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively and > 10000 nM for IGF-IR, PDGFR, AURORA2, PKA, PKB α , p38 α , MK2 and MK3). Antitumor agent; inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.PHA-665752 hydrate поставщик
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