半岛bd体育手机客户端 说明
生化/生理作用
XL019 is an ATP-binding site-targeting, orally active JAK2 subtype-selective Janus kinase inhibitor (IC50 in nM = 2.2/JAK2 vs. 134.3/JAK1, 214.2/JAK3, 348.3/TYK2) with much reduced or little activity against 116 other kinases (IC50 in nM = 125.4/PDGFRB, 139.7/FLT3, 225.8/c-KIT, 313.8/p70S6K, 370/MLK1, 375.4/IKKbeta, 483.6/KDR, 546.7/PDGFRA, 554.5/FLT4, 910.5/FLT; IC50 >1 μM toward remaining 106 kinases), CYP (1A2, 2C9, 2D6, 3A4 IC50 ≥20 μM), hERG (IC50 = 16 μM), and P-glycoprotein (IC50 >20 μM). XL019 effectively inhibits cellular STAT1/STAT3 phosphorylation both in HEL92.1.7 cultures (IC50 in nM = 386.4/pStat1 and 695/pStat3) and in HEL92.1.7 xenograft-derived tumor in micein vivo(oral ED50 in mg/kg = 42/pStat1 and 210/pStat3) with significant HEL92.1.7 tumor suppression efficacy in mice (by 60% and 70% on day 14, respectively, with 200 and 300 mg/kg bid p.o. dosage).
基本信息
| 经验(实验)分子式 | C25H28N6O2 |
| 分子量 | 444.53 |
| MDL编号 | MFCD24386874 |
半岛bd体育手机客户端 性质
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL |
| 储存温度 | 2-8℃ |
| SMILES string | O=C(NC1=CC=C(C=C1)C2=NC(NC3=CC=C(C=C3)N4CCOCC4)=NC=C2)[C@H]5NCCC5 |
安全信息
| 象形图 |  |
| 警示用语： | Danger |
| 危险声明 | H372 |
| 预防措施声明 | P260 - P264 - P270 - P314 - P501 |
| 危险分类 | STOT RE 1 Oral |
| 靶器官 | Central nervous system |
| 储存分类代码 | 6.1D - Non-combustible, acute toxic Cat.3 / toxic hazardous materials or hazardous materials causing chronic effects |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
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