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WZ3146

产品号 S1170 公司名称 Selleck Chemicals
CAS号 1214265-56-1 公司网站 http://www.selleckchem.com
分子式 C24H25ClN6O2 电 话 (877) 796-6397
分子量 464.9473 传 真 (832) 582-8590
纯 度 电子邮件 sales@selleckchem.com
保 存 -20°C Chembase数据库ID: 72554

产品价格信息

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产品别名

标题
WZ3146
IUPAC标准名
N-{3-[(5-chloro-2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)oxy]phenyl}prop-2-enamide
IUPAC传统名
N-{3-[(5-chloro-2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)oxy]phenyl}prop-2-enamide

产品登记号

CAS号 1214265-56-1

产品性质

作用靶点 EGFR
成盐信息 Free Base
溶解度 DMSO
保存条件 -20°C

产品详细信息

详细说明 (English)
Research Area
Description Cancer
Biological Activity
Description WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM, respectively.
Targets EGFR L858R EGFR E746_A750 EGFR L858R/T790M EGFR E746_A750/T790M
IC50 2 nM 2 nM 5 nM 14 nM [1]
In Vitro WZ3146 significantly suppresses the growth of EGFR mutation containing cell lines with IC50 of 3 nM in EGFR Del E746_A750 containing HCC827 cells, 15 nM in EGFR Del E746_A750 containing PC9 cells, 29 nM in EGFR L858R/T790M containing H1975 cells and 3 nM in EGFR Del E746_A750/T790M containing PC9 GR cells. [1]
In Vivo
Clinical Trials
Features Mutant-selective, irreversible
Protocol
Kinase Assay [1]
In-vitro inhibitory enzyme kinetic assays The assays are carried out in triplicate using the ATP/NADH coupled assay system in a 96-well format. The final reaction mixture contains 0.5 mg/mL Bovine Serum Albumin (BSA), 2 mM MnCl2, 1 mM phospho(enol) pyruvic acid (PEP), 1 mM TCEP, 0.1 M Hepes 7.4, 2.5 mM poly-[Glu4Tyr1] peptide, 1/50 of the final reaction mixture volume of pyruvate kinase/lactic dehydrogenase enzymes from rabbit muscle, 0.5 mM NADH, 0.5 μM EGFR kinase, 100 μM ATP and varied amount of WZ3146. WZ3146 and ATP are mixed and made separate stock from the mixture with all other ingredients and added last to the latter to start the reaction. Steady state initial velocity data are drawn from the slopes of the A340 curves.
Cell Assay [1]
Cell Lines NSCLC and Ba/F3 cells
Concentrations 0-10 μM
Incubation Time 72 hours
Methods Growth and inhibition of growth is assessed by MTS assay. NSCLC or Ba/F3 cells are exposed to treatment for 72 hours and the number of cells used per experiment is determined empirically. All experimental points are set up in six to twelve wells and all experiments are repeated at least three times. The data is graphically displayed using GraphPad Prism version 5.0 for Windows. The curves are fitted using a non-linear regression model with a sigmoidal dose response.
References
[1] Zhou W, et al. Nature, 2009, 462(7276), 1070-1074.