H3B-5942, CAS 2052128-15-9

Formulation: A crystalline solid

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

Purity: ≥98%

Formula Markup: C31H34N4O2

Formula Weight: 494,6

Shelf life (days): 1460

CAS Number: 2052128-15-9

Notes: 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.

• Artikelnummer: CAY31454-25
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 31454-25
• Green Labware: Nein
• Verpackungseinheit: 25 mg
• Mengeneinheit: STK