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CAS No. | 1213269-23-8 | Cat. No. | BCP02515 |
Name | WZ4002 | ||
Synonyms | WZ 4002;WZ-4002; | ||
SMILES | |||
Chemical Name | |||
Formula | C25H27ClN6O3 | M. Wt | 494.99 |
Purity | 98% | Storage | Store at 4-8°C |
Description | WZ4002 inhibits other EGFR genotypes E746_A750 and E746_A750/T790M with IC50 of 2 and 6 nM. Besides, WZ4002 suppresses widetype ERBB2 with an IC50 of 32 nM. WZ4002 inhibits EGFR, AKT and ERK1/2 phosphorylation in NSCLC cell lines and WZ4002 prevents of EGFR phosphorylation in NIH-3T3 cells expressing different EGFR T790M mutant alleles. For WZ4002, kinases that exhibited greater than 95% inhibition relative to the DMSO control at 10 μM are selected for measurement of their dissociation constants. WZ4002, which possesses an ortho-methoxy group at the C2-aniline substituent, is more selective for EGFR compared to WZ3146. WZ4002 is 100-fold less effective at inhibiting phosphorylation of WT EGFR compared to the quinazoline inhibitors. Similarly, WZ4002 prevents EGFR kinase activity of recombinant L858R/T790M protein more potently than of WT EGFR, while the opposite is observed with HKI-272 and gefitinib.In addition, the phosphorylated EGFR of Src TKI-resistant H1975 cells, as well as HCC8 |
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