N-(3-((5-Chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)thio)phenyl)acrylami

Name	WZ8040
Synonyms	CS-471 WZ8040 WZ-8040 WZ 8040 N-(3-(5-chloro-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-ylthio)phenyl)acrylamide N-(3-((5-Chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)thio)phenyl)acrylami N-[3-[[5-Chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]thio]phenyl]-2-propenamide 2-Propenamide, N-[3-[[5-chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]thio]phenyl]- N-[3-[[5-Chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]thio]phenyl]-2-propenamide WZ8040
CAS	1214265-57-2

Molecular Formula	C24H25ClN6OS
Molar Mass	481.01
Density	1.37
pKa	12.94±0.70(Predicted)
Storage Condition	-20℃
In vitro study	The inhibitory effect of WZ8040 on mutant EGFR T790M is much higher than that of wild-type EGFR, and the inhibitory effect on EGFR T790M is more than 30 to 100 times that of naphthyridine EGFR inhibitors such as CL-387785 and HKI-272, the inhibitory effect on wild-type EGFR was 100 times lower than that of the naphthyridine EGFR inhibitor. WZ8040 can effectively inhibit HCC827 (EGFR Del E746_A750), PC9 (EGFR Del E746_A750), H3255 (EGFR L858R), H1975 (EGFR L858R/T790M) and PC9gr (EGFR Del E746_A750/T790M) were grown, and their IC50 were 1 nM, 6 nM, 66 nM, 9 nM and 8 nM, respectively. WZ8040 weakly inhibits HCC827 GR (EGFR E746_A750/MET amp), H1819 (ERBB2 amp), Calu-3 (ERBB2 amp), H1781 (ERBB2 Ins G776V, C) and HN11 (EGFR & ERBB2 wild type), their IC50 were> 3.3 μm, 738 nM, 915 nM, 744 nM and 1.82 M. WZ8040 doses up to 10 μm were non-toxic to A549 (KRAS mutant) or H3122 (EML4-ALK) cells.

Last Update：2024-01-02 23:10:35

biological activity	WZ8040 is a novel, mutation-selective, irreversible inhibitor of EGFRT790M, there was no inhibition of ERBB2 phosphorylation (T798I).
characteristics	WZ8040 is an inhibitor of mutant EGFR T790M rather than wild-type EGFR.

Last Update：2024-04-09 02:00:14

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Product Name: WZ8040 Visit Supplier Webpage Request for quotation
CAS: 1214265-57-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

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N-(3-((5-Chloro-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)thio)phenyl)acrylami Request for Quotation