|
ChemicalBook Optimization Suppliers |
|
| 化学名: | フェドラチニブ | | 英語化学名: | Fedratinib | | 别名: | N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide;TG-101348;N-TERT-BUTYL-3-(5-METHYL-2-(4-(2-(PYRROLIDIN-1-YL)ETHOXY)PHENYLAMINO)PYRIMIDIN-4-YLAMINO)BENZENESULFONAMIDE;SAR-302503;BenzenesulfonaMide, N-(1,1-diMethylethyl)-3-[[5-Methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]aMino]-4-pyriMidinyl]aMino]-;TG101348 (SAR302503);TG101348/TG-101348;SAR302503/TG101348 | | CAS番号: | 936091-26-8 | | 分子式: | C27H36N6O3S | | 分子量: | 524.68 | | EINECS: | | | カテゴリ情報: | Inhibitor;Inhibitors;JAK;STAT | | Mol File: | 936091-26-8.mol |  |
| 融点 | 180-182°C | | 沸点 | 713.7±70.0 °C(Predicted) | | 比重(密度) | 1.247 | | 貯蔵温度 | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C | | 溶解性 | DMSO (Slightly), Methanol (Slightly) | | 外見 | Beige powder. | | 酸解離定数(Pka) | 11.95±0.50(Predicted) | | 色 | White to Off-White | | CAS データベース | 936091-26-8 |
| | フェドラチニブ Usage And Synthesis |
| 効能 | 抗悪性腫瘍薬, ヤヌスキナーゼ (JAK) 阻害薬 | | 使用 | TG101348 is a selective inhibitor of JAK2 tyrosine kinase. Potent JAK2 inhibitor. | | 使用 | A potent, highly selective and ATP-competitive JAK2 inhibitor with an IC50 of 3 nM for JAK2 and JAK2V617F. | | 定義 | ChEBI: N-tert-butyl-3-[[5-methyl-2-[4-[2-(1-pyrrolidinyl)ethoxy]anilino]-4-pyrimidinyl]amino]benzenesulfonamide is a sulfonamide. | | 生物活性 | tg101348, also known as sar302503, is a potent and selective inhibitor of janus kinase 2 (jak2), one member of a family of 4 cytoplasmic tyrosine kinases including janus kinase 1(jak1), jak2, janus kinase 3 (jak3) and tyrosine kinase 2 (tyk2), with the inhibition constant ic50 of 3 nm. comparing to other close related kinases, the selectivity of tg101348 for jak2 is 35- and 334-fold stronger than that for jak3 and jak1 respectively. tg10348 is capable of inducing apoptosis in hel cells as well baf/3 cells harboring jak2v617 mutation and inhibiting hematopoietic progenitor colony formation and erythroid engraftment in samples from polycythemia vera (pv) patients.srdan verstovsek. therapeutic potential of jak2 inhibitors. hematology am soc hematol educ program 2009:636-642 | | target | JAK2 |
|