EGFR/CDK2-IN-5 is a potent dual inhibitor of EGFR and CDK2, with IC50 values of 17.30 nM and 212.10 nM, respectively. It can also inhibit EGFRT790M with an IC50 of 123.8 nM and demonstrates significant anticancer activity. This compound induces cell cycle arrest in the G1 and S phases and promotes apoptosis (apoptosis), characterized by increased levels of caspase-3/9 and Bax and decreased levels of Bcl-2. EGFR/CDK2-IN-5 is applicable in research related to lung cancer, breast cancer, and leukemia.

CDK2:212.10 nM

EGFR/CDK2-IN-5 (compound 7c) demonstrates broad-spectrum effectiveness across various cancer cell lines, showing significant potency against HCT-116 and LOX-IMVI cells with IC 50 values of 11.3 and 20.03 μM, respectively, while exhibiting lower cytotoxicity in normal WI-38 and Vero cells (IC 50 > 50 μM). In HCT-116 cells, EGFR/CDK2-IN-5 at 11.3-20.03 μM for 24 hours induces G1 phase arrest, and in LOX-IMVI cells, it causes S phase arrest, leading to apoptosis in both cell types. Additionally, at 5.65 μM for 24 hours, EGFR/CDK2-IN-5 reduces the expression of EGFR, pEGFR, pCDK2, and CDK2 proteins in HCT-116 cells. At a concentration of 11.3 μM for 48 hours, it also enhances the gene expression levels of caspase-3/9 and Bax and increases the BAX/Bcl-2 ratio, while decreasing Bcl-2 gene expression in HCT-116 cells.