Product Name: WZ-4002

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CAT#: A-1344


  Synonym:WZ-4002,

WZ-4002 Chemical Structure
WZ-4002 chemical structure


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Biological Activity
WZ4002 is EGFR inhibitor against EGFR T790M (mutation of the gatekeeper T790 residue) which is detected in 50% of clinically resistant patients to gefitinib or erlotinib. WZ4002 has a basic chemical framework (covalent pyrimidine) which is different from that of other EGFR inhibitors. This agent is 30- to 100-fold more potent against EGFR T790M, and up to 100-fold less potent against wildtype EGFR, than quinazoline-based EGFR inhibitors (HKI-272 and CL-387,785) in vitro.
WZ 4002 is an inhibitor of EGFR phosphorylation in a variety of cancer cell lines including NIH-3T3 and H1975 cells. WZ 4002 is a potent inhibitor of EGFR, exhibiting an IC50 = 2 nM. This induces apoptosis in the cell due to the blocking of signal transduction from EGFR.
Technical Data
Formula:    C25H27ClN6O3
M.Wt:     494.97
CAS#:     213269-23-8
Purity:     >99%
Solubility : DMSO
Storage Conditions :Room temperature, or -20ºC for 2 year.

Reference




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