XL019

产品名称：

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

产品介绍：

产品说明

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 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).

基本信息

经验(实验)分子式	C₂₅H₂₈N₆O₂
分子量	444.53
MDL编号	MFCD24386874

产品性质

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