货号	规格	价格	上海	北京	珠海	重庆	武汉
S88556-1mg促销	≥98%	￥412.00 ￥320.00 S88556-1mg ￥320.00 现货	3 3	-	-	-	-
S88556-5mg促销	≥98%	￥1330.00 ￥1070.00 S88556-5mg ￥1070.00 现货	6 6	-	-	-	-
S88556-10mg促销	≥98%	￥1850.00 ￥1480.00 S88556-10mg ￥1480.00 现货	4 4	-	-	-	-
S88556-25mg促销	≥98%	￥3700.00 ￥2960.00 S88556-25mg ￥2960.00 现货	7 7	-	-	-	-
S88556-50mg促销	≥98%	￥6180.00 ￥4940.00 S88556-50mg ￥4940.00 现货	1 1	-	-	-	-
S88556-100mg促销	≥98%	￥10300.00 ￥8230.00 S88556-100mg ￥8230.00 现货	1 1	-	-	-	-

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产品描述：

H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERαWT or ERα mutations

靶点：

ERαY537S:0.41 nM (Ki);ERαWT:1 nM (Ki);EstrogenReceptor/ERR; Estrogen/progestogenReceptor

体外研究：

H3B-5942 is a selective and irreversible estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 elevates ERα protein level distinct from SERMs/SERD, blocks ERα-dependent transcription in breast cancer cells. H3B-5942 (0.01-10 μM) reduces ERα target gene GREB1 in MCF7-ERαWT, various MCF7-ERαMUT lines, and the PDX-ERαY537S/WT line. H3B-5942 also decreases proliferation of MCF7-Parental, MCF7-LTED-ERαWT, and MCF7-LTED-ERαY537C lines with GI50s of 0.5, 2, and 30 nM, respectively. H3B-5942 (10-25 nM) in combination with CDK4/6 inhibitors (≥25 pM) has synergic inhibitory effect on multiple cell lines bearing ERαWT or clinically frequent ERα mutations

体内研究：

H3B-5942 (1, 3, 10, or 30 mg/kg, p.o, q.d. for 17 days) dose-dependently inhibits tumor growth in MCF7 xenograft model in athymic female nude mice. H3B-5942 (3, 10, 30, 100, and 200 mg/kg, p.o, q.d.) exhibits similar anti-tumor activity in the ERαY537S/WT ST941 model in athymic female nude mice. Animal Model: MCF7 xenograft model in athymic female nude mice Dosage: 1, 3, 10, or 30 mg/kg Administration: P.O. once a day (q.d.×1) for 17 days Result: Exhibited tumor growth inhibition (TGI) on day 17 of 19%, 41%, 68%, and 83%, respectively.

参考文献：

1. Puyang X, et al. Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer. Cancer Discov. 2018 Sep;8(9):1176-1193.

溶解性：

Soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.022 ml	10.109 ml	20.217 ml
5 mM	0.404 ml	2.022 ml	4.043 ml
10 mM	0.202 ml	1.011 ml	2.022 ml
50 mM	0.04 ml	0.202 ml	0.404 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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