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BMS 599626 dihydrochloride is a potent and selective inhibitor of EGFR and ErbB2 with IC50 values of 22 and 32 nM, respectively [1].

The epidermal growth factor receptor (EGFR) is the cell-surface receptor for epidermal growth factor and plays an important role in tumor invasion and cancer cell proliferation. Receptor tyrosine-protein kinase erbB-2 (ErbB2) is a human epidermal growth factor receptor and plays a critical role in breast cancer.

BMS 599626 dihydrochloride is a potent and selective EGFR and ErbB2 inhibitor. BMS-599626 inhibited HER4 with IC50 value of 190 nM. In Sal2, N87 and GEO tumor cells, BMS-599626 inhibited phosphorylation of HER1 and HER2 in a dose-dependent way and inhibited cell proliferation. In AU565 breast cancer cells, BMS-599626 (1μM) inhibited HER1/HER2 heterodimer formation [1]. In tumor cells that forming HER1/HER2 heterodimers, BMS-599626 inhibited heterodimerization [2].

In the L2987 human lung tumors xenograft models, BMS-599626 (60 mg/kg) inhibited and delayed tumor growth in a dose-dependent way [1].

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