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首页-小分子抑制剂&激动剂-Epigenetics-HDAC-SBI-46
SBI-46

Chemical Structure : SBI-46

CAS No.:

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SBI-46 (SBI 46)

货号: PC-20402Not For Human Use, Lab Use Only.

SBI-46 (SBI 46) is an antiandrogen-equipped histone deacetylase (HDAC) inhibitor, strongly binds to androgen receptor (AR, IC50=8.4 nM) and potently inhibited HDACs and the proliferation of AR+ CRPC.

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

    生物&药学活性

    SBI-46 (SBI 46) is an antiandrogen-equipped histone deacetylase (HDAC) inhibitor, strongly binds to androgen receptor (AR, IC50=8.4 nM) and potently inhibited HDACs and the proliferation of AR+ CRPC.
    SBI-46 showed much tighter affinity than enzalutamide (MDV-3100, Cat# PC-45932).
    SBI-46 possessed potent anti-HDAC activity against HDAC1 and HDAC6 with IC50 of 66 and 15 nM, respectively, much less potent against HDAC8 (IC50=3,500 nM).
    SBI-46 potently inhibited cell growth of AR+ (LNCaP IC50=500 nM), and AR+ splice variants (AR-SV) and CRPC cells (C4-2B-IC50=480 nM and 22Rv1 IC50=560 nM), without effects against AR-null PC-3 cells.
    SBI-46 caused a dose-dependent upregulation of acetylated H4 and tubulin in LNCaP cells.
    SBI-46 inhibited cytoplasmic and nuclear expressions of AR and AR-V, downregulated DHT-induced AR expression in CRPC cells.
    SBI-46 (20 mg/kg, orally, five days/week for four weeks) potently suppressed PCa xenografts tumor growth in nude mice.

    物理化学性质&存储条件

    分子量 629.62
    分子式 C30H31F4N7O4
    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

    8-(4-(4-((3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-2,4-dioxoimidazolidin-1-yl)methyl)-3-fluorophenyl)-1H-1,2,3-triazol-1-yl)-N-hydroxyoctanamide

    参考文献

    1. Chandrasekaran B, et al. Cancers (Basel). 2023 Mar 15;15(6):1769.

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