A selective estrogen receptor covalent antagonist; covalently modifies cysteine 530 in the ligand binding domain of wild-type ERα and ERαY537S; inhibits expression of the ERα target genes GREB1 and TFF1 in MCF-7 cells overexpressing wild-type ERα (IC50s = 2.74 and 1.3 nM

H3B-5942 – 10 mg

Brand:
Cayman
CAS:
2052128-15-9
Storage:
-20
UN-No:
Non-Hazardous - /

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 α (ERα) and ERαY537S. HB-5942 inhibits expression of the ERα target genes GREB1 and TFF1 in MCF-7 cells overexpressing wild-type ERα (IC50s = 2.74 and 1.3 nM, respectively) or the mutant receptors ERαY537S (IC50s = 29.38 and 19.4 nM, respectively), ERαY537N (IC50s = 8.14 and 6.1 nM, respectively), ERαY537C (IC50s = 12.19 and 9.5 nM, respectively), or ERαD538G (IC50s = 24.87 and 4 nM, respectively), which are active independent of estradiol. It inhibits the growth of MCF-7 cells overexpressing wild-type ERα or ERαY537S (GI50s = 1.3 and 8.3 nM, respectively). H3B-5942 reduces tumor growth in an MCF-7 mouse xenograft model and an ERαY537S/WT ST941 patient-derived xenograft (PDX) mouse model in a dose-dependent manner.  

 

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SKU: 31454 - 10 mg Category:

Description

A selective estrogen receptor covalent antagonist; covalently modifies cysteine 530 in the ligand binding domain of wild-type ERα and ERαY537S; inhibits expression of the ERα target genes GREB1 and TFF1 in MCF-7 cells overexpressing wild-type ERα (IC50s = 2.74 and 1.3 nM, respectively), ERαY537S (IC50s = 29.38 and 19.4 nM, respectively), ERαY537N (IC50s = 8.14 and 6.1 nM, respectively), ERαY537C (IC50s = 12.19 and 9.5 nM, respectively), or ERαD538G (IC50s = 24.87 and 4 nM, respectively); inhibits the growth of MCF-7 cells overexpressing wild-type ERα or ERαY537S (GI50s = 1.3 and 8.3 nM, respectively); reduces tumor growth in an MCF-7 mouse xenograft model and an ERαY537S/WT ST941 PDX mouse model in a dose-dependent manner

Formal name: (2E)-4-[[2-[4-[(1E)-1-(1H-indazol-5-yl)-2-phenyl-1-buten-1-yl]phenoxy]ethyl]amino]-N,N-dimethyl-2-butenamide

Synonyms: 

Molecular weight: 494.6

CAS: 2052128-15-9

Purity: ≥98%

Formulation: A crystalline solid

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