HER2-IN-22 is a potent and selective HER2 inhibitor with an IC50 value of 215 μM. It exhibits cytotoxic activity against various tumor cells and can induce apoptosis. HER2-IN-22 significantly suppresses tumor growth in mice and can be utilized for research in HER2+ breast cancer and other tumors.

HER2:215 μM

HER2-IN-22 (compound 3f) demonstrates average GI 50 values of 1.9, 2.5, and 2.3 μM against leukemia, central nervous system, and breast cancer cell lines in the NCI 60 cell line panel. At a concentration of 10 μM for 30 minutes, it achieves 88% inhibition of HER2. The compound has an IC 50 value of 215 μM for HER2 kinase inhibition when tested from 0.05 to 250 μM over 30 minutes. For antiproliferative activity, HER2-IN-22 exhibits high potency against BT474, BT549, and ZR-75-30 cell lines with IC 50 values of 323.3, 282.6, and 271.7 nM, respectively, over a period of 72 hours at concentrations ranging from 0 to 50 μM. Additionally, in BT474 cells, HER2-IN-22 induces necrosis to a maximum level of 10.5% at 10 μM over 72 hours.

HER2-IN-22 (compound 3f) (10 mg/kg; i.p.; single dose) demonstrated antitumor activity in a mouse breast cancer model.