H3B-5942 (H3B5942) is a selective, irreversible (covalent) and orally bioavailable estrogen receptor antagonist with antitumor activity (better than fulvestrant). Acts by inactivating both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERαWT or ERα mutations.
纯度:≥98%
CAS:2052128-15-9