Catalog No.: PC-35365Not For Human Use, Lab Use Only.
H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA) with Ki 1 nM and 0.41 nM for wild-type and mutant ERα Y537S respectively, covalently targeting Cys530.
H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA) with Ki 1 nM and 0.41 nM for wild-type and mutant ERα Y537S respectively, covalently targeting Cys530.
H3B-5942 demonstrates potent ERα antagonist activity in vitro and in vivo.
H3B-5942 covalently inactivates both wild-type and mutant ERα by targeting Cys530 and enforcing a unique antagonist conformation.
H3B-5942 demonstrates significant single-agent antitumor activity in xenograft models representing ERαWT and ERα Y537S breast cancer, which is superior to fulvestrant (Cat# PC-21622).
