EGFR/CDK2-IN-5 

EGFR/CDK2-IN-5 is a potent dual EGFR and CDK2 inhibitor with IC₅₀s of 17.30 and 212.10 nM, respectively. EGFR/CDK2-IN-5 also inhibits EGFR^T790M with an IC₅₀ of 123.8 nM. EGFR/CDK2-IN-5 exhibits potent anticancer activity. EGFR/CDK2-IN-5 induces G1 and S cell cycle arrest and apoptosis, accompanied by increased levels of caspase-3/9 and Bax, as well as decreased Bcl-2 levels. EGFR/CDK2-IN-5 can be used for the research of cancers, such as lung cancer, breast cancer, and leukemia^[1].

EGFR/CDK2-IN-5 (compound 7c) (48 h) exhibits broad-spectrum activity in a panel of cancer cells, displays potent activity against HCT-116 and LOX-IMVI with IC₅₀s of 11.3 and 20.03 μM, while showing low cytotoxicity on normal cells WI-38 and Vero cells (IC50 > 50 μM) ^[1].
EGFR/CDK2-IN-5 (11.3-20.03 μM, 24 h) induces G1 phase arrest in HCT-116 and S phase arrest in LOX-IMVI cells, and induces apoptosis in both cells^[1].
EGFR/CDK2-IN-5 (5.65 μM, 24 h) reduces the expression of EGFR, pEGFR, CDK2, and pCDK2 in HCT-116 cells.^[1].
EGFR/CDK2-IN-5 (11.3 μM, 48 h) increases gene expression levels of caspase-3/9 and Bax, and BAX/Bcl-2 ratio, while decreasing Bcl-2 mRNA levels in HCT-116 cells^[1].

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

508.61

C₃₁H₃₂N₄O₃

N#CC1=C(NCC2=CC(CN3CCN(C)CC3)=C(O)C(OC)=C2)OC(C4=CC=CC=C4)=C1C5=CC=CC=C5

Room temperature in continental US; may vary elsewhere.

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

• [1]. Osman EEA, et al. New 2-benzylideneamino-4,5-diphenylfuran-3‑carbonitrile derivatives and their benzylamino analogues: Synthesis, in vitro cytotoxicity, protein kinase inhibitory activity and in silico insights. Bioorg Chem. Published online November 21, 2025.  [Content Brief]