BC-N102 is a first-in-class novel small molecule inhibitor for targeting oncogenic and hormonal signaling in ER-positive breast cancer.
BC-N102 exhibits anticancer activity against breast cancer cell lines via interfering with cell cycle regulatory proteins and hormonal receptors signaling in vitro (IC50=0.04-10 uM), no significant activities against a normal breast cell line.
BC-N102 exhibits potent antitumor activity at tolerated doses in an ER+ human xenograft breast cancer model.
BC-N102 induces arrest of the cell cycle at G0/G1 phase, downregulates the expression of CDK2 and CDK4 independent of the ER in breast cancer cell lines.
