EGFR-IN-1 (compound 24) is an orally active and irreversibleL858R/T790M mutant selectiveEGFRinhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistantEGFRL858R, T790M with 100-fold selectivity over wild-typeEGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity^[1].

EGFR-IN-1 (10 μM; 72 hours) displays strong antiproliferative activity against the H1975 and HCC827 cells with IC50s of 4 and 28 nM, respectively^[1].
EGFR-IN-1 inhibits p-EGFR in H1975 and HCC827 cells with IC₅₀s of 4 and 9 nM, respectively. EGFR-IN-1 highly selective against a panel of 100 kinases^[1].

EGFR-IN-1 (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight^[1].
EGFR-IN-1 evaluates in a time course PD experiment upon oral dosing at 30 mg/kg. EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h^[1].

514.58

C₂₈H₃₀N₆O₄

1625677-63-5

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