EGFR-IN-77 

EGFR-IN-77 (Compound 4a) is a selective EGFR^T790M/L858R inhibitor, with an IC₅₀ of 0.101 μM against EGFR^T790M/L858R, 0.477 μM against EGFR^L858R, and 1.771 μM against wild-type EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFR^T790M/L858R non-small cell lung cancer. EGFR-IN-77 can be used for the research of EGFR^L858R/T790M double-mutant non-small cell lung cancer^[1].

EGFR-IN-77 inhibits purified TL double mutant EGFR kinase with an IC₅₀ of 0.101 μM, L858R mutant EGFR kinase with an IC₅₀ of 0.477 μM, and WT EGFR kinase with an IC₅₀ of 1.771 μM, exhibiting 17.52-fold selectivity for TL EGFR over WT EGFR^[1].
EGFR-IN-77 inhibits proliferation of H1975 (TL EGFR) NSCLC cells with an IC₅₀ of 0.184 μM, PC9 (L858R EGFR) cells with an IC₅₀ of 0.137 μM, and H292 (WT EGFR) cells with an IC₅₀ of 8.321 μM, exhibiting 45.27-fold selectivity for H1975 cells over H292 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

472.54

C₂₆H₂₈N₆O₃

2222930-49-4

O=C(NC1=CC(NC2=NC(C3=CN(C)C4=C3C=CC=C4)=CC=N2)=C(C=C1N(CCO)C)OC)C=C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. An B, et al. The discovery of a potent and selective third-generation EGFR kinase inhibitor as a therapy for EGFR L858R/T790M double mutant non-small cell lung cancer. Eur J Med Chem. 2019 Dec 1;183:111709.  [Content Brief]