EGFR-IN-60 

EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR^WT, EGFR^T790M, EGFR^L858R and JAK3 with IC₅₀s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR^T790M mutation (IC₅₀=1.32 µM) over A431 cells overexpressing EGFR^WT (IC₅₀=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio^[1].

EGFR-IN-60 (compound 7d) (3.25-88.46 μM, 48 hours) shows well antitumor activity against hepatocellular (HepG2), colorectal (HCT-116) and breast (MCF-7) cancer cells^[1].
EGFR-IN-60 (compound 7d) (0.49-86.4 μM, 48 hours) shows cytotoxic activity against cancer cells^[1].
EGFR-IN-60 (compound 7d) (0-5.27 μM, 24 hours) induces an increase in G2/M phase cells and induces apoptosis in HepG2, HCT-116, and MCF-7 cell lines^[1].
EGFR-IN-60 (compound 7d) (0 µM, 10 µM, 24 hours) can induce apoptosis through up-regulation of Bax and down-regulation of Bcl-2^[1].

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

535.47

C₂₈H₂₈Cl₂N₆O

2699877-43-3

O=C1C2=C(NC(N=CN(/N=C/C3=CC=C(N(C)C)C=C3)C4=N)=C4C2C5=CC=CC(Cl)=C5Cl)CC(C)(C)C1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Mennatallah A Shaheen, et al. Design, synthesis and biological evaluation of new series of hexahydroquinoline and fused quinoline derivatives as potent inhibitors of wild-type EGFR and mutant EGFR (L858R and T790M). Bioorg Chem. 2020 Dec;105:104274.  [Content Brief]