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首页-抗体药物偶连体和PROTACs-PROTAC-ERD-1233
ERD-1233

Chemical Structure : ERD-1233

CAS No.: 3098604-77-1

ERD-1233 (ERD1233)

货号: PC-24557Not For Human Use, Lab Use Only.

ERD-1233 is a potent and orally efficacious PROTAC degrader of estrogen receptor α (ERα) with DC50 of 0.9 nM in MCF-7 cell line, Dmax=100%.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    ERD-1233 is a potent and orally efficacious PROTAC degrader of estrogen receptor α (ERα) with DC50 of 0.9 nM in MCF-7 cell line, Dmax=100%.
    ERD-1233 potently and effectively reduces the ERα protein in vitro and achieves excellent oral bioavailability in mice and rats.
    Oral administration of ERD-1233 effectively reduces ER protein in ER+ tumors and achieves tumor regression in the ER wild-type MCF-7 xenograft tumor model and strong tumor growth inhibition in the ESR1Y537S mutated model in mice.

    物理化学性质&存储条件

    分子量 807.99
    分子式 C49H53N5O6
    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

    (3S)-3-((5aR)-7-((8-(4-((1R,2S)-6-Hydroxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenyl)-1-oxa-8-azaspiro[4.5]decan-3-yl)methyl)-1-oxo-1,3,5,5a,6,7,8,9-octahydro-2H-pyrazino[1′,2′:4,5][1,4]oxazino[2,3-e]isoindol-2-yl)piperidine-2,6-dione

    参考文献

    1. Acharyya RK, et al. J Med Chem. 2024 Nov 14;67(21):19010-19037.

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