WZ4002 Inhibitor CAS No. 1213269-23-8

Cat. No.	Name	Size	Price
KI1177	WZ4002	10 mg	$192
	WZ4002	50 mg	$592
	WZ4002	100 mg	$1072
	WZ4002	200 mg	$1712

Chemical Characteristic

Product Name	WZ4002
CAS No.	1213269-23-8
Molecular Weight	494.97
Formula	C₂₅H₂₇ClN₆O₃
Chemical Name	N-(3-(5-chloro-2-(2-methoxy-4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yloxy)phenyl)acrylamide
Smiles	C(=O)(C=C)Nc1cc(ccc1)Oc1nc(ncc1Cl)Nc1c(cc(cc1)N1CCN(CC1)C)OC
Chemical Structure

Biological activities

WZ4002 is a potent EGFR inhibitor. WZ4002 is a third-generation inhibitor. WZ4002 inhibits EGFR^L858R and EGFR^L858R/T790M with an IC50 of 2 and 8 nM, respectively. In contrast, the IC50 of WZ4002 is 32 nM against wild type ERBB2. WZ4002 inhibits EGFR phosphorylation. WZ4002 suppresses the growth of EGFR^T790M-containing cell lines including Ba/F3 cell line.^[1] It is also reported that WZ4002 markedly decreases the phosphorylation levels of EGFR in H1975 SR cells. WZ4002 similarly inhibits the phosphorylation levels of EGFR and its main downstream molecules, Akt and ERK 1/2, in H1975 SR cells, as well as HCC827 cells in suspension.^[2] WZ4002 prevents the proliferation of H1975 cells with a gatekeeper T790M mutation, but does not suppress the growth of HCC827ER and PC-9/HGF cells.^[3] WZ4002 significantly regresses tumor growth compared to vehicle alone in both T790M-containing murine models with Ba/F3 cells and PC9 cells.^[1]

Protocols

In vivo: WZ4002 is dissolved in 10% 1-methyl-2-pyrrolidinone: 90% PEG-300.^[1]

References

[1] Zhou W, et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009, 462(7276): 1070-1074. [2] Sakuma Y, et al. WZ4002, a third-generation EGFR inhibitor, can overcome anoikis resistance in EGFR-mutant lung adenocarcinomas more efficiently than Src inhibitors. Lab Invest. 2012, 92(3): 371-383. [3] Nakagawa T, et al. Combined therapy with mutant-selective EGFR inhibitor and Met kinase inhibitor for overcoming erlotinib resistance in EGFR-mutant lung cancer. Mol Cancer Ther. 2012, 11(10): 2149-2157.

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