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H3B-5942

    
≥98%

H3B-5942

源叶(MedMol)
S88556 一键复制产品信息
2052128-15-9
C31H34N4O2
494.63
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
S88556-1mg促销
≥98%

¥412.00 ¥320.00

3 - - - -
S88556-5mg促销
≥98%

¥1330.00 ¥1070.00

6 - - - -
S88556-10mg促销
≥98%

¥1850.00 ¥1480.00

4 - - - -
S88556-25mg促销
≥98%

¥3700.00 ¥2960.00

7 - - - -
S88556-50mg促销
≥98%

¥6180.00 ¥4940.00

1 - - - -
S88556-100mg促销
≥98%

¥10300.00 ¥8230.00

1 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
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

质检证书(COA)

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