1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  2. HSP Apoptosis
  3. Ganetespib

Ganetespib  (Synonyms: STA-9090)

目录号: HY-15205 纯度: 99.84%
COA 产品使用指南

Ganetespib (STA-9090) 是一种热休克蛋白 90 (HSP90) 抑制剂,在多种血液和实体肿瘤细胞系中表现出有效的细胞毒性。Ganetespib 通过抑制 HIF-1α 和 STAT3 对大肠癌具有抗血管生成作用。

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Ganetespib Chemical Structure

Ganetespib Chemical Structure

CAS No. : 888216-25-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥660
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1 mg ¥318
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5 mg ¥600
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10 mg ¥800
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25 mg ¥1200
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50 mg ¥1500
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100 mg ¥2400
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200 mg ¥3400
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500 mg ¥5500
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 30 篇科研文献

WB
IHC

    Ganetespib purchased from MCE. Usage Cited in: Int J Biochem Cell Biol. 2019 Jan;106:35-45.  [Abstract]

    Levels of HSP70, and phosphorylation and total protein of p38, ERK, JNK, JAK2, STAT3, IκB-α and p65 in total cell lysates are analysed using Western blotting with or without ganetespib (100 nM).

    Ganetespib purchased from MCE. Usage Cited in: Int J Biochem Cell Biol. 2019 Jan;106:35-45.  [Abstract]

    Confocal immunofluorescence microscopy is performed on cultures that are immunoreacted with antibodies against HSP90β and phospho-Tyr705-STAT3 at 6-h recovery after heat shock with or without ganetespib (100 nM) and HSP90β esiRNA.

    Ganetespib purchased from MCE. Usage Cited in: Anticancer Res. 2019 Apr;39(4):1767-1775.  [Abstract]

    Ganetespib suppresses epidermal growth factor receptor (EGFR) and its related downstream pathway molecules in non-small cell lung cancer cells with acquired resistance to EGFR-tyrosine kinase inhibitor. Cells are treated with the indicated concentration of ganetespib for 24 h, and lysates were analyzed by western blot. AKT: protein kinase B; EMT: epithelial-mesenchymal transition; MET: met proto-oncogene; amp: amplification; MAPK: mitogen-activated protein kinase.

    Ganetespib purchased from MCE. Usage Cited in: Cancer Cell. 2018 Sep 10;34(3):411-426.e19.  [Abstract]

    Immunoblot of HSP70 expression in RD cells after treatment with Ganetespib (GSP) alone or CPT-11+NSC-67574.

    Ganetespib purchased from MCE. Usage Cited in: Cell Stress Chaperones. 2018 Sep;23(5):1137-1142.  [Abstract]

    Western blot analysis of human bladder cancer cell lysates (T24) treated with DMSO, the Hsp90 inhibitor STA9090, the Hsp70 inhibitors VER155008, and MAL3-101 or combinations of the various inhibitors. The blot is probed with a keratin 9 mouse monoclonal antibody

    Ganetespib purchased from MCE. Usage Cited in: Massachusetts Institute of Technology, University of Texas at Dallas. 2018 Jun.

    Immunoblot of HEK293T-REx cells inducibly expressing dn-cHSF1 following pretreatment with vehicle or dox (18 h; 1 pg/mL) and then HSR activation by treatment with arsenite (6 h; 100 pM) or STA-9090 (6 h; 100 nM).

    Ganetespib purchased from MCE. Usage Cited in: Massachusetts Institute of Technology, University of Texas at Dallas. 2018 Jun.

    Immunoblot of HEK293T-Rex cells upon treatment with increasing concentrations of the HSP90 inhibitor STA-9090.

    Ganetespib purchased from MCE. Usage Cited in: ACS Chem Biol. 2016 Jan 15;11(1):200-10.  [Abstract]

    Protein level by immunoblotting for HSR target proteins.

    Ganetespib purchased from MCE. Usage Cited in: Sci Rep. 2015 Aug 3;5:12728.  [Abstract]

    Ganetespib decreases the DYRK1A protein level. 293T cells are transiently transfected with an expression vector for 3xFLAG-DYRK1A. At 24 h after transfection, the cells are treated with Ganetespib (100 nM) and collected 0 and 8 h after treatment. Total cell lysates are subjected to SDS-PAGE followed by Western blot analysis using antibodies against FLAG and GAPDH. In the control group (DMSO), expression of 3xFLAG-DYRK1A increases at 8 h compared to 0 h, and Ganetespib suppresses this increase of

    Ganetespib purchased from MCE. Usage Cited in: Oncotarget. 2015 Nov 24;6(37):39821-38.  [Abstract]

    J82 cells are treated with 1 μM STA9090 and 50 μM VER155008 as mono or dual therapy for the time indicated. Lysates are prepared and Western blots probed for cell cycle markers.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3[1][2][3][4][5][6].

    IC50 & Target[1]

    HSP90

     

    体外研究
    (In Vitro)

    Ganetespib causes depletion of receptor tyrosine kinases, extinguishing of downstream signaling, inhibition of proliferation and induction of apoptosis with IC50 values ranging 2-30 nM in genomically-defined NSCLC cell lines. Ganetespib is also approximately 20-fold more potent in isogenic Ba/F3 pro-B cells rendered IL-3 independent by expression of EGFR and ERBB2 mutants[1]. Ganetespib exhibits potent in vitro cytotoxicity in a range of solid and hematologic tumor cell lines, induces the degradation of known Hsp90 client proteins, displays superior potency to the ansamycin inhibitor 17-allylamino-17-demethoxygeldanamycin (17-AAG)[2]. Ganetespib is a potent HSP90 inhibitor, and shown to kill canine tumor cell lines in vitro[3]. Ganetespib possesses superior JAK/STAT inhibitory activity to both P6 and 17-AAG in terms of potency or duration of response in the HEL92.1.7 cells[4].

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

    体内研究
    (In Vivo)

    Ganetespib (125 mg/kg, i.v.) accumulates in tumors relative to normal tissues and displays greater in vivo efficacy than 17-AAG without increased toxicity and inhibits proliferation and induces apoptosis in parallel with EGFR depletion in NCI-H1975 xenografts[1]. Ganetespib (100, 125, 150 mg/kg, i.v.) shows potent antitumor efficacy in solid and hematologic xenograft models of oncogene addiction, as evidenced by significant growth inhibition and/or regressions[2].

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

    Clinical Trial
    分子量

    364.40

    Formula

    C20H20N4O3

    CAS 号
    性状

    固体

    颜色

    White to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (274.42 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.7442 mL 13.7212 mL 27.4424 mL
    5 mM 0.5488 mL 2.7442 mL 5.4885 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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6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: 15% Cremophor EL    85% Saline

      Solubility: 10 mg/mL (27.44 mM); 悬浊液; 超声助溶

    • 方案 二

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.86 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    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)。
    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: 99.84%

    参考文献
    Kinase Assay
    [1]

    Exponentially growing cells are processed in lysis buffer (20 mM HEPES, pH 7.4, 1 mM EDTA, 5 mM MgCl2, 100 mM KCl) and incubated with increasing concentrations of 17-AAG or ganetespib for 30 min at 4°C, and incubated with biotin-GM linked to Dynabeads MyOne Streptavidin T1 magnetic beads for 1 h at 4°C. Beads are washed three times in lysis buffer and heated for 5 min at 95°C in SDS-PAGE sample buffer. Samples are resolved on 4-12% Bis-Tris gradient gel and Western blots are performed using an anti-HSP90 antibody.

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

    Cell Assay
    [2]

    Cells are grown in 96-well plates based on optimal growth rates determined empirically for each line. Twenty-four hours after plating, cells are treated with the indicated compounds or controls for 72 hours. AlamarBlue is added (10% v/v) to the cells, and the plates are incubated for 3 hours and, then, subjected to fluorescence detection. For the comparative viability/apoptosis assay, NCI-H1975 cells are treated with escalating concentrations of ganetespib for the indicated time periods and subjected to viability analysis via CellTiter Fluor and apoptosis via Caspase Glo 3/7.

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

    Animal Administration
    [1]

    Mice: NCI-H1975 or HCC827 cells are cultured as above and 0.5-1×107 cells are mixed with 50% RPMI 1640/50% Matrigel and subcutaneously injected into the flanks of SCID mice. For efficacy studies, animals with 100-200 mm3 tumors are then randomized into treatments groups of eight. Tumor volumes (V) are calculated by the equation V=0.5236×L×W×T (Length, width, and thickness). Animals are treated by intravenous bolus tail vein injection at 10 mL/kg with ganetespib formulated in 10/18 DRD (10% DMSO, 18% Cremophor RH 40, 3.6% dextrose and 68.4% water). As a measurement of in vivo efficacy, the relative size of treated and control tumors [(%T/C) value] is determined from the change in average tumor volumes of each drug-treated group relative to the vehicle-treated group, or itself in the case of tumor regression. Body weights are monitored daily. For biomarker studies, mice bearing NCI-H1975 xenografts are treated with either a single dose of vehicle or ganetespib, or with 5 daily doses of vehicle or ganetespib, in groups of 3 or 8, and harvested at various time points. Tumors are excised and flash frozen in liquid nitrogen for preparation of protein lysates or fixed in 10% neutral buffered formalin for immunohistochemistry.

    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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6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 2.7442 mL 13.7212 mL 27.4424 mL 68.6059 mL
    5 mM 0.5488 mL 2.7442 mL 5.4885 mL 13.7212 mL
    10 mM 0.2744 mL 1.3721 mL 2.7442 mL 6.8606 mL
    15 mM 0.1829 mL 0.9147 mL 1.8295 mL 4.5737 mL
    20 mM 0.1372 mL 0.6861 mL 1.3721 mL 3.4303 mL
    25 mM 0.1098 mL 0.5488 mL 1.0977 mL 2.7442 mL
    30 mM 0.0915 mL 0.4574 mL 0.9147 mL 2.2869 mL
    40 mM 0.0686 mL 0.3430 mL 0.6861 mL 1.7151 mL
    50 mM 0.0549 mL 0.2744 mL 0.5488 mL 1.3721 mL
    60 mM 0.0457 mL 0.2287 mL 0.4574 mL 1.1434 mL
    80 mM 0.0343 mL 0.1715 mL 0.3430 mL 0.8576 mL
    100 mM 0.0274 mL 0.1372 mL 0.2744 mL 0.6861 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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    目录号:
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