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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Estrogen Receptor/ERR-H3B-6545
H3B-6545

Chemical Structure : H3B-6545

CAS No.: 2052130-80-8

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H3B-6545 (H3B6545)

货号: PC-49171Not For Human Use, Lab Use Only.

H3B-6545 is a potent, covalent antagonist of both wild-type and mutant estrogen receptor alpha (ERα), shows antiproliferative activity for ERαWT and ERαY537S overexpressing MCF7 cells with or without H524 L ESR1 mutation with low nM IC50 values.

规格 价格 库存 数量
5 mg ￥2480 In stock
10 mg ￥4280 In stock
25 mg ￥7580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

H3B-6545 is a potent, covalent antagonist of both wild-type and mutant estrogen receptor alpha (ERα), shows antiproliferative activity for ERαWT and ERαY537S overexpressing MCF7 cells with or without H524 L ESR1 mutation with low nM IC50 values.
H3B-6545 also binds ERα/β with comparable affinities without impacting the function of other closely related nuclear hormone receptors (PRα, PRβ, AR, GR, and MR).
H3B-6545 demonstrates potent antagonist activity across a panel of ERαWT/MUT cell lines and SERM activity in bone and uterine tissues.
H3B-6545 demonstrates significant activity and superiority over standard-of-care fulvestrant across a panel of ERαWT and ERαMUT palbociclib sensitive and resistant models.
H3B-6545 (3-30 mg/kg) demonstrates single-agent antitumor activity in ERαWT and ERαMUT xenograft models.

物理化学性质&存储条件

分子量 567.589
分子式 C30H29F4N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(2E)-N,N-Dimethyl-4-[[2-[[5-[(1Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenyl-1-buten-1-yl]-2-pyridinyl]oxy]ethyl]amino]-2-butenamide

参考文献

1. Craig Furman, et al. Mol Cancer Ther. 2022 Jun 1;21(6):890-902.

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