WZ4002 manufacturers and suppliers

WZ4002 suppliers

WZ4002

CAS:: 1213269-23-8

MF:: C25H27ClN6O3

MW:: 494.97

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Properties

Density: 1.314

storage temp.: Store at -20°C

solubility: ≥24.7 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH

form: solid

pka: 12.78±0.70(Predicted)

Safety Information

Use

WZ4002 also inhibit other EGFR genotypes. For instance, the IC50 is 2nM and 6nM respectively when it acts on E746_A750 and E746_A750/T790M. Besides, the IC50 is 32nM when it acts on wild-type EGFR. It could inhibit the phosphorylation of EGFR, AKT and ERK1/2 when it acts on non-small cell lung cancer (NSCLC). WZ4002 also could inhibit the phosphorylation of EGFR when it acts on NIH-3T3 cells expressing different EGFRT790M mutant alleles. The dissociation constant of kinase was 95% higher when in the test when WZ4002 involved than that in the test DMSO involved instead. Because in aniline substitution in the C2 WZ4002 could obtain a methoxy group when it acts on EGFR, thus its more effective when it acts on EGFR than WZ3146. Compared with the quinazoline inhibitors, the efficiency of WZ4002 is 100 times lower than when it acts on wild-type EGFR. The inhibitory effect of WZ4002 on EGFR kinase activity of recombinant L858R/T790M protein is much higher than restrainable wild-type EGFRs. However HKI-272 and Gefitinib are happened to have opposite inhibitory effect compared with WZ4002. In addition, phosphorylation of EGFR in H1975 and HCC827 cells of anti-Src TKI could be completely inhibited by third-generation EGFR TKI and WZ4002.

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