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WZ8040EGFR T790M inhibitor,irreversible amd potent

WZ8040

Catalog No. A1393
Size Price Stock Qty
10mM (in 1mL DMSO) $230.00 In stock
5mg $120.00 In stock
25mg $360.00 In stock
100mg $800.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

WZ8040

Biological Activity

Description WZ8040 is an irreversible inhibitor of EGFR T790M with IC50 value of <10nM.
Targets EGFR T790M          
IC50 <10nM          

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Chemical Properties

Cas No. 1214265-57-2 SDF Download SDF
Chemical Name N-[3-[5-chloro-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]oxyphenyl]prop-2-enamide
Canonical SMILES CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC=C(C(=N3)SC4=CC=CC(=C4)NC(=O)C=C)Cl
Formula C24H25ClN6OS M.Wt 481.01
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

WZ8040 is a novel, irreversible mutant-selective EGFR kinase inhibitor that specifically inhibits phosphorylation of EGFRT790M.

WZ8040 shows to suppress the growth of EGFR T790M containing cell lines as well as inhibit phosphorylation of EGFR in the Non–Small-Cell Lung Cancer (NSCLC) cells. WZ8040 was identified from the screen that possessed up to a 300-fold lower IC50 against the PC9GR cells compared to clinical stage inhibitors such as HKI-272 [1].

References:
[1] Zhou W1, Ercan D, Chen L, Yun CH, Li D, Capelletti M, Cortot AB, Chirieac L, Iacob RE, Padera R, Engen JR, Wong KK, Eck MJ, Gray NS, Jänne PA. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature. 2009 Dec 24;462(7276):1070-4. doi: 10.1038/nature08622.