THIQ40

THIQ 40 (THIQ40) is a potent, orally available ERα antagonist and selective estrogen receptor degrader (SERD) with IC50 of 17 nM (ERα binding) and 30 nM (ERα transcription), IC50 of 0.9 nM (ERα degradation); potently inhibits insulin driven proliferation in MCF-7 cells with IC50 of 2.1 nM, downregulate ERα protein levels and inhibit MCF-7 proliferation in an estradiol-independent manner; demonstrated SERD activity at tolerated and efficacious exposures in vivo.

References 1. Burks HE, et al. J Med Chem. 2017 Apr 13;60(7):2790-2818. View Related Products by Target Estrogen Receptor/ERR