PF-6274484

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].

Product Specifications

CAS Number

[1035638-91-5]

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pf-6274484.html

Purity

98.76

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

C=CC(NC1=CC2=C(NC3=CC(Cl)=C(F)C=C3)N=CN=C2C=C1OC)=O

Molecular Formula

C18H14ClFN4O2

Molecular Weight

372.78

Precautions

H302, H315, H319

References & Citations

[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.