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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-WZ4002
WZ4002

Chemical Structure : WZ4002

CAS No.: 1213269-23-8

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WZ4002 (WZ 4002;WZ-4002)

货号: PC-42841Not For Human Use, Lab Use Only.

WZ4002 is a potent, mutant-selective, covalent EGFR inhibitor with IC50 of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746-A750 and EGFRE746-A750/T790M, respectively.

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5 mg (Free Sample) ￥280 In stock
25 mg ￥1280 In stock
50 mg ￥1980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

WZ4002 is a potent, mutant-selective, covalent EGFR inhibitor with IC50 of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746-A750 and EGFRE746-A750/T790M, respectively.
WZ4002 increases cellular potency correlated with inhibition of EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines and EGFR phosphorylation in NIH-3T3 cells expressing different EGFRT790M mutant alleles.
WZ4002 inhibits EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR.
WZ4002 suppresses the growth of erlotinib-resistant tumors caused by gatekeeper T790M mutation combined with Met kinase inhibitor E-7050 in vivo.

物理化学性质&存储条件

分子量 494.9733
分子式 C25H27ClN6O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-Propenamide, N-[3-[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]oxy]phenyl]-

参考文献

1. Sakuma Y, et al. Lab Invest. 2012 Mar;92(3):371-83.

2. Zhou W, et al. Nature. 2009 Dec 24;462(7276):1070-4.

3. Nakagawa T, et al. Mol Cancer Ther. 2012 Oct;11(10):2149-57.

4. Ercan D, et al. Cancer Discov. 2012 Oct;2(10):934-47.

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