An inhibitor of mutant EGFRs (IC50s = 2-2

WZ3146 – 1 mg

Brand:
Cayman
CAS:
1214265-56-1
Storage:
-20
UN-No:
Non-Hazardous - /

WZ3146 is an irreversible inhibitor of mutant EGF receptors (EGFRs) with IC50 values ranging from 2 to 2,740 nM in Ba/F3 cells.{27829} It is selective for EGFR mutants including EGFRL858R and EGFRDel E746_A750 (IC50s = 2 nM for both) over wild-type EGFR (IC50 = 750 nM in HN11 cells) but also inhibits ERBB2Ins G776V,C and wild-type ERBB2 (IC50s = 10 and 24 nM, respectively, in Ba/F3 cells). However, it does not inhibit the ERBB2T7981 gatekeeper mutant. WZ3146 (10-1,000 nM) decreases phosphorylation of EGFR, AKT, and ERK1/2 in H1975 non-small cell lung cancer (NSCLC) cells in a concentration-dependent manner. It inhibits proliferation of PC-9 NSCLC and gefitinib-resistant PC-9 GR cells (EC50s = 15 and 3 nM, respectively).{41787}  

 

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SKU: 23440 - 1 mg Category:

Description

An inhibitor of mutant EGFRs (IC50s = 2-2,740 nM); selective for EGFR mutants including EGFRL858R and EGFRDel E746_A750 (IC50s = 2 nM for both) over wild-type EGFR (IC50 = 750 nM); inhibits ERBB2Ins G776V,C and wild-type ERBB2 (IC50s = 10 and 24 nM, respectively, in Ba/F3 cells) but not the ERBB2 gatekeeper mutant; decreases phosphorylation of EGFR, AKT, and ERK1/2 in H1975 NSCLC cells at 10-1,000 nM; inhibits proliferation of PC-9 and PC-9 GR cells (EC50s = 15 and 3 nM, respectively)

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

Synonyms: 

Molecular weight: 465

CAS: 1214265-56-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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