PF-6274484 Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMF: 33 mg/ml; DMSO: 25 mg/ml

form 

A crystalline solid

color 

Light yellow to orange

PF-6274484 Usage And Synthesis

Description

PF-6274484 is an irreversible EGFR kinase inhibitor that covalently reacts with active-site cysteine residues in the ATP binding pocket. PF-6274484 inhibits autophosphorylation of both wild type and mutant EGFR in tumor cells with IC50 values of 5.8 nM and 6.6 nM, respectively.

Uses

PF-6274484 is a potent EGFR inhibitor with Kis of 0.14 nM and 0.18 nM for EGFR-L858R/T790M and WT EGFR, respectively. PF-6274484 inhibits EGFR-L858R/T790M autophosphorylation in H1975 tumor cells and EGFR WT in A549 tumor cells with IC50s of 6.6 and 5.8 nM, respectively[1].

IC 50

EGFR (WT): 0.18 nM (Ki); EGFR^L858R/T790M: 0.14 nM (Ki)

References

[1] Schwartz PA, et al. Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance. Proc Natl Acad Sci U S A. 2014;111(1):173-178. DOI:10.1073/pnas.1313733111

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