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  • 17-AAG
  • 坦螺旋霉素;替拉替尼;17-烯丙基胺格尔德霉素;Tanespimycin; NSC 330507; CP 127374; 17AAG; 17 AAG; KOS 953
  • 货号: abs810017
    CAS号: 75747-14-7
    分子式: C31H43N3O8
    分子量: 585.7
    产品说明书
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    货号-规格 货期 价格 数量
    abs810017-5mg 现货 ¥599.00
    - +
    abs810017-10mg 现货 ¥666.00
    - +
    abs810017-25mg 现货 ¥1199.00
    - +
    abs810017-50mg 现货 ¥1790.00
    - +
    abs810017-100mg 现货 ¥2960.00
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    大包装询价
    产品描述
    描述

    Tanespimycin (17-AAG)是一种有效的HSP90抑制剂,无细胞试验中IC50为5 nM,作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。

    纯度
    >98 %
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
    基本信息
    别名
    坦螺旋霉素;替拉替尼;17-烯丙基胺格尔德霉素;Tanespimycin; NSC 330507; CP 127374; 17AAG; 17 AAG; KOS 953
    外观
    紫色到略带紫色的红色固体
    可溶性/溶解性
    DMSO : 58.6 mg/mL (100 mM)
    生物活性
    靶点
    HSP90
    In vitro(体外研究)
    17-AAG, an analog of geldanamycin, exhibits greater than 100 times higher binding affinity for Hsp90 derived from HER-2-overexpressing cancer cells (BT474, N87, SKOV3 and SKBR3) or BT474 breast carcinoma cells with IC50 values of 5-6 nM. 17-AAG causes the degradation of HER2, HER3, Akt, and both mutant and wild-type androgen receptor (AR), leading to the RB-dependent G1 growth arrest of prostate cancer cells such as LNCaP, LAPC-4, DU-145, and PC-3 with IC50 values of 25-45 nM. In addition to inducing apoptosis of Ba/F3 cells transformed with wild-type BCR-ABL with an IC50 of 5.2 μM, 17-AAG has the ability to induce apoptosis of cells transformed with imatinib mesylate-resistant T315I and E255K BCR-ABL mutants with IC50 values of 2.3 μM and 1.0 μM, respectively, by inducing the degradation of both wild-type BCR-ABL protein and mutants.
    In vivo(体内研究)
    17-AAG displays significantly higher binding affinity for Hsp90 from 3T3-src, B16 or CT26 xenografts in nude mice with IC50 values of 8-35 nM as compared with that from the normal tissues with IC50 values of 200-600 nM. Administration of 17-AAG (~50 mg/kg) causes significant decline in AR, HER2, HER3, and Akt expression in a dose-dependent manner with >50% decline at dose of 50 mg/kg, resulting in the dose-dependent inhibition of androgen-dependent (CWR22) and -independent (CWR22R and CWRSA6) prostate cancer xenografts growth by 67%, 80% and 68% at dose of 50 mg/kg, respectively.
    参考文献
    参考文献
    [1] Kamal A, et al. Nature, 2003, 425(6956), 407-410.
    [2] Solit DB, et al. Clin Cancer Res, 2002, 8(5), 986-993.
    [3] Gorre ME, et al. Blood, 2002, 100(8), 3041-3044.
    温馨提示:本产品仅作科研实验使用,不支持临床等研究
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