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首页-小分子抑制剂&激动剂-Proteasome/Ubiquitin-Heat Shock Protein (HSP)-STA-1474
STA-1474

Chemical Structure : STA-1474

CAS No.: 1118915-78-8

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STA-1474 (STA1474)

货号: PC-20709Not For Human Use, Lab Use Only.

STA-1474 is a water soluble prodrug of Ganetespib (STA 9090), which is a potent, second generation small-molecule inhibitor of HSP90 (IC50=4 nM).

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

    生物&药学活性

    STA-1474 is a water soluble prodrug of Ganetespib (STA 9090), which is a potent, second generation small-molecule inhibitor of HSP90 (IC50=4 nM).
    STA-1474 promoted loss of cell viability, inhibition of cell proliferation and induction of apoptosis in osteosarcoma (OSA) cell lines.
    STA-1474 and its active metabolite STA-9090 also demonstrated increased potency compared to 17-AAG.
    STA-1474 exhibited selectivity for OSA cells versus normal canine osteoblasts, and HSP90 co-precipitated with co-chaperones p23 and Hop in canine OSA cells but not in normal canine osteoblasts.
    STA-1474 downregulated the expression of p-Met/Met, p-Akt/Akt and p-STAT3.
    STA-1474 induced tumor regression, caspase-3 activation and downregulation of p-Met/Met and p-Akt/Akt in OSA xenografts.

    物理化学性质&存储条件

    分子量 444.38
    分子式 C20H21N4O6P
    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

    5-hydroxy-2-isopropyl-4-(4-(1-methyl-1H-indol-5-yl)-5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)phenyl dihydrogen phosphate

    参考文献

    1. Lin TY, et al. Exp Hematol. 2008 Oct;36(10):1266-77.

    2. McCleese JK, et al. Int J Cancer. 2009 Dec 15;125(12):2792-801.

    3. Bansal H, et al. Blood. 2010 Nov 25;116(22):4591-9.

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