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WZ8040

规格或纯度: ≥98%
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货号 (SKU) 包装规格 是否现货 价格 数量
W126471-1mg
1mg 期货 Stock Image
W126471-5mg
5mg 期货 Stock Image
W126471-10mg
10mg 期货 Stock Image
W126471-25mg
25mg 期货 Stock Image
W126471-50mg
50mg 期货 Stock Image
W126471-100mg
100mg 期货 Stock Image
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EGFR inhibitor

基本描述

英文别名 WZ8040|1214265-57-2|WZ-8040|N-(3-((5-chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)thio)phenyl)acrylamide|N-[3-[5-chloro-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]sulfanylphenyl]prop-2-enamide|WZ 8040|SCHEMBL93523|MLS006011280
规格或纯度 ≥98%
英文名称 WZ8040
生化机理 WZ8040 is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wild-type EGFR, than quinazoline-based EGFR inhibitors such as CL-387785 and HKI-272. WZ8040 treatment potently inhibits the growth of HCC827 (EGFR Del E746_A750), PC9 (EGFR Del E746_A750), H3255 (EGFR L858R), H1975 (EGFR L858R/T790M), and PC9 GR (EGFR Del E746_A750/T790M) with IC50 of 1 nM, 6 nM, 66 nM, 9 nM, and 8 nM, respectively. WZ8040 weakly inhibits the growth of HCC827 GR (EGFR E746_A750/MET amp), H1819 (ERBB2 amp), Calu-3 (ERBB2 amp), H1781 (ERBB2 Ins G776V, C), and HN11 (EGFR & ERBB2 WT) with IC50 of >3.3 μM, 738 nM, 915 nM, 744 nM, and 1.82 μM, respectively. WZ8040 is not toxic up to 10 μM against A549 (KRAS mutant) or H3122 (EML4-ALK) cells.
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍

WZ8040是突变选择型不可逆EGFRT790M抑制剂,对ERBB2磷酸化(T798I)无抑制性。A potent inhibitor of EGFR T790M

WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I).
A potent inhibitor of EGFR T790M

名称和标识符

IUPAC Name N-[3-[5-chloro-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]sulfanylphenyl]prop-2-enamide
INCHI InChI=1S/C24H25ClN6OS/c1-3-22(32)27-18-5-4-6-20(15-18)33-23-21(25)16-26-24(29-23)28-17-7-9-19(10-8-17)31-13-11-30(2)12-14-31/h3-10,15-16H,1,11-14H2,2H3,(H,27,32)(H,26,28,29)
InChi Key KIISCIGBPUVZBF-UHFFFAOYSA-N
Canonical SMILES CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)SC4=CC=CC(=C4)NC(=O)C=C)Cl
Isomeric SMILES CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)SC4=CC=CC(=C4)NC(=O)C=C)Cl
PubChem CID 44607531
分子量 481.02

化学和物理性质

溶解性 DMSO ≥93mg/mL Water <1.2mg/mL Ethanol ≥2.8mg/mL

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