Catalog No.: PC-49172Not For Human Use, Lab Use Only.
H3B-6545 hydrochloride is a potent, covalent antagonist of both wild-type and mutant estrogen receptor alpha (ERα), shows antiproliferative activity for ERαWT and ERαY537S overexpressing MCF7 cells with or without H524 L ESR1 mutation with low nM IC50 values.
H3B-6545 hydrochloride is a potent, covalent antagonist of both wild-type and mutant estrogen receptor alpha (ERα), shows antiproliferative activity for ERαWT and ERαY537S overexpressing MCF7 cells with or without H524 L ESR1 mutation with low nM IC50 values.
H3B-6545 also binds ERα/β with comparable affinities without impacting the function of other closely related nuclear hormone receptors (PRα, PRβ, AR, GR, and MR).
H3B-6545 demonstrates potent antagonist activity across a panel of ERαWT/MUT cell lines and SERM activity in bone and uterine tissues.
H3B-6545 demonstrates significant activity and superiority over standard-of-care fulvestrant across a panel of ERαWT and ERαMUT palbociclib sensitive and resistant models.
H3B-6545 (3-30 mg/kg) demonstrates single-agent antitumor activity in ERαWT and ERαMUT xenograft models.
