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Description: H3B-5942 is a selective, irreversible (covalent) and orally bioavailable estrogen receptor antagonist, inactivating both wild-type and mutant ERalpha by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERalpha target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERalphaWT or ERalpha mutations.
References: Puyang X, et al. Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERalphaWT and ERalphaMUT Breast Cancer. Cancer Discov. 2018 Sep; 8(9):1176-1193.
Related CAS #: 2052132-46-2 (HCl) 2052128-15-9 (free base)
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