An inhibitor of mutant EGFR (IC50s = 2-306 in Ba/F3 cells); selective for EGFR mutants

WZ8040 – 5 mg

Brand:
Cayman
CAS:
1214265-57-2
Storage:
-20
UN-No:
Non-Hazardous - /

WZ8040 is an inhibitor of mutant EGF receptors (EGFRs) with IC50 values ranging from 2 to 306 nM in Ba/F3 cells.{27829} It is selective for EGFR mutants, including the EGFRDel E746_A750 and EGFRL858R mutations conferring gefitinib sensitivity and the EGFRDel E746_A750/T790M mutation conferring gefitinib resistance (IC50s = 2, 6, and 6 nM in Ba/F3 cells), over wild-type EGFR (IC50 = 1,820 nM in HN11 cells) but also inhibits ERBB2Ins G776V,C and wild-type ERBB2 (IC50s = 20 and 32 nM, respectively, in Ba/F3 cells). WZ8040 inhibits proliferation of PC-9 cells harboring the EGFRDel E746_A750 mutation and gefitinib-resistant PC-9 GR cells harboring the EGFRT790M resistant allele (EC50s = 6 and 8 nM, respectively).{41787}  

 

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SKU: 30062 - 5 mg Category:

Description

An inhibitor of mutant EGFR (IC50s = 2-306 in Ba/F3 cells); selective for EGFR mutants, including the EGFRDel E746_A750 and EGFRL858R mutations conferring gefitinib sensitivity and the EGFRDel E746_A750/T790M mutation conferring gefitinib resistance (IC50s = 2, 6, and 6 nM in Ba/F3 cells), over wild-type EGFR (IC50 = 1,820 nM in HN11 cells); inhibits ERBB2Ins G776V,C and wild-type ERBB2 (IC50s = 20 and 32 nM, respectively, in Ba/F3 cells); inhibits proliferation of PC-9 cells harboring the EGFRDel E746_A750 mutation and gefitinib-resistant PC-9 GR cells harboring the EGFRT790M resistant allele (EC50s = 6 and 8 nM, respectively)

Formal name: N-[3-[[5-chloro-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]thio]phenyl]-2-propenamide

Synonyms: 

Molecular weight: 481

CAS: 1214265-57-2

Purity: ≥98%

Formulation: A crystalline solid

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