您的位置：首页 > 产品中心 > 945755-56-6， XL019
XL019
产品别名
945755-56-6
XL019
(S)-N-(4-(2-(4-Morpholinophenylamino)pyrimidin-4-yl)phenyl)pyrrolidine-2-carboxamide
N-(4-{2-[(4-Morpholin-4-ylphenyl)amino]pyrimidin-4-yl}phenyl)-L-prolinamide
(2S)-N-[4-[2-[[4-(4-Morpholinyl)phenyl]amino]-4-pyrimidinyl]phenyl]-2-pyrrolidinecarboxamide
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C25H28N6O2 |
| Molecular weight | 444.53 |
| MDL number | MFCD24386874 |
| Biochem/physiol Actions【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 mice in 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). |
产品性质
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL |
| storage temp.【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
| Pictograms【象形图】 | GHS08 |
| Signal word【警示用语：】 | Danger |
| Hazard Statements | H372 |
| Precautionary Statements | P260 - P264 - P270 - P314 - P501 |
| Hazard Classifications【危险分类】 | STOT RE 1 Oral |
| Target Organs【靶器官】 | Central nervous system |
| Storage Class Code【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 |
