Chemical Structure : H3B-6545
CAS No.: 2052130-80-8
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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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.
分子量 | 567.589 | |
分子式 | C30H29F4N5O2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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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 |
1. Craig Furman, et al. Mol Cancer Ther. 2022 Jun 1;21(6):890-902.
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