EGFR/HER2-IN-6 (compound 43) is a dual EGFR/HER2 and DHFR inhibitor with potent activity against EGFR kinase, HER2 kinase, and DHFR, characterized by IC50 values of 0.122 μM, 0.078 μM, and 0.585 μM, respectively. This compound displays notable anticancer properties in various cancer cell lines, while demonstrating a favorable safety profile and selectivity indices. Consequently, EGFR/HER2-IN-6 holds promise as a valuable tool in cancer research [1].

EGFR/HER2-IN-6 (0-100 μM; 72 h) shows remarkable broad spectrum cytotoxic potency, and the cytotoxic potency against MCF7 cells is more potent than SOR [1]. EGFR/HER2-IN-6 (0-20 μM; 0-48 h) affects cell cycle and indeces apoptosis of MCF-7 cells [1]. Cell Cytotoxicity Assay [1] Cell Line: HepG2 hepatocellular carcinoma, MCF7 breast cancer, HCT-116 colorectal carcinoma, PC-3 prostate, Hea cervical epithelioid carcinoma cell lines and WI-38 fetal lung fibroblast cells Concentration: 0-100 μM Incubation Time: 72 hours Result: Exhibited cytotoxic potency to HepG2, MCF7, HCT-116, PC-3 and Hela cell lines with IC 50 s of 12.18, 2.37, 16.18, 18.39 and 9.43 μM. Showed a lower cytotoxic potency to WI-38 normal cell line with an IC 50 value of 36.84 μM. Apoptosis Analysis [1] Cell Line: MCF-7 breast cancer cell line Concentration: 0-20 μM Incubation Time: 0-48 hours Result: Through arrested cell cycle at G1/S and G1 phases and induced apoptosis in MCF-7 cells rather than necrosis to achieve anti-breast cancer activity.

EGFR/HER2-IN-6 (10 mg/kg; i.p. once per day for 20days) shows anti-breast cancer activity in mice [1]. Animal Model: 8-week-old swiss albino female mice [1] Dosage: 10 mg/kg Administration: Intraperitoneal injection; 10 mg/kg once per day; for 20 days Result: Decreased tumor volume 65.3% and reduced body weight 7.4% after 20 days of treatment.