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Chemical Structure : H3B-6545
CAS No.: 2052130-80-8
Catalog No.: 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.
| 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 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 | 567.589 | |
| Formula | C30H29F4N5O2 | |
| Appearance | Solid | |
| Storage |
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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 |
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1. Craig Furman, et al. Mol Cancer Ther. 2022 Jun 1;21(6):890-902.
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