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Tanespimycin (17-AAG, KOS953)

目录号: A10010
HSP90 抑制剂
17-AAG 是一种安萨霉素类抗生素,具有抗肿瘤作用。具体来说,17-AAG 通过结合并抑制 Hsp90 来发挥作用。
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5mg
¥210.00
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10mg
¥350.00
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25mg
¥630.00
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50mg
¥1,085.00
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100mg
¥1,715.00
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200mg
¥2,415.00
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10mM * 1mL in DMSO
¥315.00
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重要通知:仅供研究使用。我们不向患者销售。

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Adooq用户使用Tanespimycin (17-AAG, KOS953)发表的1篇文献
  • Yool Lee, .et al. , Sci Adv, 2021, 7
  • 生物活性
    Discription 17-AAG is an ansamycin antibiotic which acts as an anti-tumor agent. Specifically, 17-AAG binds and inhibits Hsp90.
    Targets
    Target Value
    Cell Research
    Cell Line Type Value Description References
    In Vitro

    Hsp90 derived from tumor cells exhibits a significantly higher binding affinity—approximately 100-fold greater—for Tanespimycin compared to Hsp90 from normal cells. In vitro reconstitution of chaperone complexes with Hsp90 demonstrated an enhanced binding affinity for Tanespimycin, accompanied by an increase in ATPase activity [1]. Tanespimycin induces the degradation of HER2, Akt, and both mutant and wild-type androgen receptor (AR), leading to retinoblastoma-dependent G1 cell cycle arrest in prostate cancer cells [2]. Furthermore, the combination of Tanespimycin and Trastuzumab in ErbB2-overexpressing breast cancer cell lines results in synergistic effects, including enhanced ubiquitination, downregulation of ErbB2 from the cell surface, and subsequent lysosomal degradation [3].

    References
    1. Kamal A, et al. A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors. Nature. 2003 Sep 25;425(6956):407-10.
    2. Solit DB, et al. 17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts.Clin Cancer Res, 2002, 8(5), 986-993.
    3. Raja SM, et al. A combination of Trastuzumab and 17-AAG induces enhanced ubiquitinylation and lysosomal pathway-dependent ErbB2 degradation and cytotoxicity in ErbB2-overexpressing breast cancer cells. Cancer Biol Ther. 2008 Oct;7(10):1630-40.
    产品信息
    目录号 A10010
    分子式 C31H43N3O8
    分子量 585.7
    CAS号 75747-14-7
    SMILES CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCC=C)C)OC)OC(=O)N)C)C)O)OC
    其他名称 Tanespimycin, NSC330507, CP 127374
    储存条件

    Store lyophilized at -20ºC, keep desiccated.
    In lyophilized form, the chemical is stable for 36 months.
    In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

    溶解性数据
    In vitro (25°C) DMSO 97 mg/mL (165.61 mM)
    Water Insoluble
    Ethanol 5 mg/mL
    In vivo 5%DMSO+corn oil 9 mg/mL
    * <1 mg/ml means slightly soluble or insoluble.
    * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
    Preparing Stock Solutions
    Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
    0.1 mM 17.07 mL 85.37 mL 170.74 mL
    0.5 mM 3.41 mL 17.07 mL 34.15 mL
    1 mM 1.71 mL 8.54 mL 17.07 mL
    5 mM 0.34 mL 1.71 mL 3.41 mL
    Useful Calculator

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