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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EGFR/ErbB1/HER1
Available Sizes
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