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  3. Tanespimycin

Tanespimycin  (Synonyms: 坦螺旋霉素; 17-AAG; NSC 330507; CP 127374)

目录号: HY-10211 纯度: 99.07%
COA 产品使用指南

Tanespimycin (17-AAG) 是有效的 HSP90 抑制剂,IC50 为 5 nM,对肿瘤细胞 HSP90 的亲和性比正常细胞高 100 倍。Tanespimycin 消耗细胞内 STK38/NDR1,并降低 STK38 激酶活性。Tanespimycin 还下调 stk38 基因表达。

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Tanespimycin Chemical Structure

Tanespimycin Chemical Structure

CAS No. : 75747-14-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥770
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5 mg ¥437
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10 mg ¥698
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25 mg ¥1100
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50 mg ¥1650
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100 mg ¥2475
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500 mg   询价  

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 35 篇科研文献

WB
IHC

    Tanespimycin purchased from MCE. Usage Cited in: Int J Mol Med. 2023 Apr;51(4):32.  [Abstract]

    Tanespimycin (17‑AAG) inhibits the levels of HSP90 and NLRP3, and decreases GSDMD expression, in MH‑S cells.

    Tanespimycin purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Mar 27;37(1):70.  [Abstract]

    Cells are first treated with commercially available HIF-1α inhibitors, including compounds targeting Top1 (Camptothecin, CPT), Top2 (VP; MX) and HSP90 (17-AAG) as well as 2-ME, and then subjected to Western blotting analysis.

    Tanespimycin purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Feb 7;9(2):165.  [Abstract]

    Western blot analysis of Hsp70 protein and Hsp90 client proteins IKK and EGFR after 24 h Tan IIA treatment. The Hsp90 inhibitor 17-AAG (10 μM) is included as a positive control

    Tanespimycin purchased from MCE. Usage Cited in: Front Mol Neurosci. 2018 Nov 6;11:401.  [Abstract]

    Effects of 17-AAG on neurogenesis 4 weeks after SAH.

    Tanespimycin purchased from MCE. Usage Cited in: Mol Cancer Ther. 2016 Sep;15(9):2107-18.  [Abstract]

    Combination of MDV3100 and 17-AAG leads to decreased AR protein level and transcriptional activity. (A&B) LNCaP (A) and C4-2 (B) cells are treated as indicated for 24 hr, followed by IB against AR, PSA and CHIP. (C&D) 22RV1 (C) and MR49F (D) cells are treated as indicated for 24 hr, followed by IB against AR and HSP90. (E) C4-2 cells are treated as indicated for 24 hr, fractionated into cytoplasm and nuclear, followed by IB against AR and Plk1.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90[1][5]. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression[3].

    IC50 & Target[5]

    HSP90

    5 nM (IC50)

    Autophagy

     

    Mitophagy

     

    体外研究
    (In Vitro)

    Tanespimycin 导致 HER2、Akt 以及突变型和野生型 AR 的降解以及前列腺癌细胞的视网膜母细胞瘤依赖性 G1 期生长停滞。Tanespimycin 抑制前列腺癌细胞系,IC50 范围为 25-45 nM (LNCaP,25 nM;LAPC-4,40 nM;DU-145,45 nM;和 PC-3,25 nM)[1]
    Tanespimycin (0.1-1 μM) 诱导过表达 ErbB2 的乳腺癌细胞几乎完全丧失 ErbB2[2]
    Tanespimycin 抑制 CCA 细胞生长并诱导 G2/M 细胞周期停滞和凋亡,同时下调 Bcl-2、Survivin 和 Cyclin B1,上调 cleaved PARP[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Tanespimycin (25 -200 mg/kg,ip) 引起前列腺癌异种移植物中 AR、HER2 和 Akt 表达的剂量依赖性下降。Tanespimycin 以足以诱导 AR、HER2 和 Akt 降解的剂量进行处理,可剂量依赖性地抑制雄激素依赖性和非依赖性前列腺癌异种移植物的生长,且无毒性[1]
    Tanespimycin (60 mg/kg) 和 Rapamycin (30 mg/kg) 通过尾静脉注射抑制 A549 和 MDA-MB-231 肿瘤生长并影响 MDA-MB-231 荷瘤动物的肿瘤治愈[4]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    585.69

    Formula

    C31H43N3O8

    CAS 号
    性状

    固体

    中文名称

    坦螺旋霉素

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 50 mg/mL (85.37 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.7074 mL 8.5369 mL 17.0739 mL
    5 mM 0.3415 mL 1.7074 mL 3.4148 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 5 mg/mL (8.54 mM); 澄清溶液

      此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 5 mg/mL (8.54 mM); 澄清溶液

      此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.07%

    参考文献
    Cell Assay
    [1]

    For the Alamar Blue proliferation assay, 2-4×103 cells are plated in 96-well plates. Later (48 h), cells are treated with Tanespimycin for 96 h or 0.01% DMSO as control. On day 4, Alamar Blue viability assay is performed as described elsewhere. IC50 and IC90s are calculated as the doses of Tanespimycin required to inhibit cell growth by 50 and 90%, respectively. Cell cycle distribution is assayed as described previously with a Becton Dickinson fluorescence-activated cell sorter and analyzed by the Cell Cycle Multicycle system.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    Tanespimycin is dissolved in an EPL vehicle. To aid in the identification of an optimal dose and schedule, nontumor bearing mice are treated by i.p. injection with 25-200 mg/kg of Tanespimycin 5 days/week for 3 weeks or by the EPL vehicle alone. Serum samples are taken from each group, and equal volumes are pooled on days 5, 10, and 15 of treatment for serum chemistry and liver function analysis. At sacrifice, plasma samples are collected for complete blood count. A gross necropsy is performed on all of the mice, and a complete necropsy, including histopathology, is performed on 1 animal/group.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7074 mL 8.5369 mL 17.0739 mL 42.6847 mL
    5 mM 0.3415 mL 1.7074 mL 3.4148 mL 8.5369 mL
    10 mM 0.1707 mL 0.8537 mL 1.7074 mL 4.2685 mL
    15 mM 0.1138 mL 0.5691 mL 1.1383 mL 2.8456 mL
    20 mM 0.0854 mL 0.4268 mL 0.8537 mL 2.1342 mL
    25 mM 0.0683 mL 0.3415 mL 0.6830 mL 1.7074 mL
    30 mM 0.0569 mL 0.2846 mL 0.5691 mL 1.4228 mL
    40 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0671 mL
    50 mM 0.0341 mL 0.1707 mL 0.3415 mL 0.8537 mL
    60 mM 0.0285 mL 0.1423 mL 0.2846 mL 0.7114 mL
    80 mM 0.0213 mL 0.1067 mL 0.2134 mL 0.5336 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
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    目录号:
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