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Chemical Structure : H3B-6545 hydrochloride
CAS No.: 2052132-51-9
Catalog No.: PC-49172Not For Human Use, Lab Use Only.
H3B-6545 hydrochloride 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $248 | In stock | |
| 10 mg | $428 | In stock | |
| 25 mg | $758 | In stock | |
| 100 mg | Get quote |
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H3B-6545 hydrochloride 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.
| M.Wt | 604.047 | |
| Formula |
C30H30ClF4N5O2 |
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| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(E)-N,N-dimethyl-4-((2-((5-((Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)pyridin-2-yl)oxy)ethyl)amino)but-2-enamide hydrochloride |
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1. Craig Furman, et al. Mol Cancer Ther. 2022 Jun 1;21(6):890-902.
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