H3B-5942

H3B-5942

CAT N°: 31454
Price:

66.00 56.10

H3B-5942 is a selective estrogen receptor covalent antagonist (SERCA).{57227} It covalently modifies cysteine 530 in the ligand binding domain of wild-type estrogen receptor ? (ER?) and ER?Y537S. HB-5942 inhibits expression of the ER? target genes GREB1 and TFF1 in MCF-7 cells overexpressing wild-type ER? (IC50s = 2.74 and 1.3 nM, respectively) or the mutant receptors ER?Y537S (IC50s = 29.38 and 19.4 nM, respectively), ER?Y537N (IC50s = 8.14 and 6.1 nM, respectively), ER?Y537C (IC50s = 12.19 and 9.5 nM, respectively), or ER?D538G (IC50s = 24.87 and 4 nM, respectively), which are active independent of estradiol. It inhibits the growth of MCF-7 cells overexpressing wild-type ER? or ER?Y537S (GI50s = 1.3 and 8.3 nM, respectively). H3B-5942 reduces tumor growth in an MCF-7 mouse xenograft model and an ER?Y537S/WT ST941 patient-derived xenograft (PDX) mouse model in a dose-dependent manner.

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