溶解性 | Soluble in DMSO (61 mg/ml at 25 °C), ethanol (15 mg/ml) with warming, DMF (~5 mg/ml), water (<1 mg/ml at 25 °C), and methanol. |
存贮条件 | 储存温度-20°C |
应用 | An inhibitor of JAK1, JAK2, and JAK3. |
产品介绍 | Ruxolitinib (INCB018424)是第一个应用于临床的、有效的、选择性的JAK1/2抑制剂,IC50为3.3 nM/2.8 nM。作用于JAK1, JAK2与 作用于JAK3相比,选择性强130倍多。 |
备注 | INCB018424 is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3. |
生化机理 | Ruxolitinib (INCB018424) is a JAK inhibitor of JAK1 (IC50 = 2.7 nM), JAK2 (IC50 = 4.5 nM), and JAK3 (IC50 = 322 nM). JAKs, or Janus-associated kinases, are tyrosine kinases found in the cytoplasm that are known to active the signaling of certain growth factor receptors and cytokines. |
别名 | (betaR)-beta-环戊基-4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-丙腈;INCB 018424;INCB018424;INCB-018424;(betaR)-beta-Cyclopentyl-4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazole-1-propanenitrile |