H3B-5942
A selective estrogen receptor covalent antagonist
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包装价格促销价数量
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1mg￥700.00560.00- +
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5mg￥2062.001650.00- +
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10mg￥3262.002610.00- +
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25mg￥6262.005010.00- +
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50mg￥10687.008550.00- +
- 货号: ajcx12948
- CAS: 2052128-15-9
- 别名:
- 分子式: C31H34N4O2
- 分子量: 494.63
- 纯度: ＞98%
- 溶解度: DMSO: 83.33 mg/mL (168.47 mM)
- 储存: Store at -20°C
- 库存: 现货
Background
H3B-5942 is a selective estrogen receptor covalent antagonist (SERCA).1 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.
1.Puyang, X., Furman, C., Zheng, G.Z., et al.Discovery of selective estrogen receptor covalent antagonists for the treatment of ERαWT and ERαMUT breast cancerCancer Discov.8(9)1176-1193(2018)
