BMS-599626 2HCL (AC480 2HCl) is a BMS-599626 derivative. BMS-599626 is an orally available and selective dual inhibitor of HER1 and HER2 with IC50s of 20 and 30 nM, respectively. BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor BMS-599626 inhibits tumor cell proliferation and has the potential to increase tumor response to radiotherapy.

HER2:30 nM, HER1:20 nM, HER4:190 nM

BMS-599626 is a potent HER inhibitor and has a higher inhibition ability than the other reported inhibitors. When tested with breast tumor cell lines (HCC202, HCC1942 and AU565) that highly expressed HER1 and HER2, BMS-599626 treatment inhibited cell proliferation, while having no effect on A2780 cells without HER1 or HER2 expression.[1]
Treated OV202 cells with BMS-599626 significantly inhibited cell proliferation and enhanced cell apoptosis by inhibiting HER.[3]
When tested with Sal2 cells expressing CD8-HER2 fusion protein, BMS-599626 treatment inhibited the receptor phosphorylation and MAPK phosphorylation with the IC50 value of 0.3 and 0.22 μM/L, respectively.[1]

In mouse models with Sal2 tumor cells xenograft, oral administration of BMS-599626 inhibited Sal2 cells growth in a dose-dependent manner and significantly delayed tumor growth at the concentration of 60 mg/kg.[1]