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

Luminespib  (Synonyms: VER-52296; AUY922; NVP-AUY922)

目录号: HY-10215 纯度: 99.74%
COA 产品使用指南

Luminespib (VER-52296) 是有效的 HSP90 抑制剂,抑制 HSP90α 和 HSP90β 的 IC50 分别为 7.8 和 21 nM。

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Luminespib Chemical Structure

Luminespib Chemical Structure

CAS No. : 747412-49-3

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3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550
In-stock
1 mg ¥250
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5 mg ¥498
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10 mg ¥700
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25 mg ¥1500
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50 mg ¥2250
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100 mg ¥3500
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200 mg ¥5338
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Customer Review

    Luminespib purchased from MCE. Usage Cited in: Blood. 2018 Jul 19;132(3):307-320.  [Abstract]

    K562, KCL22 and HL60 are treated with the indicated (cytotoxic) concentration of Amidopyrine (AX) and AUY922 for 48h and later protein lysates are subjected to immunoblot analysis.

    Luminespib purchased from MCE. Usage Cited in: Clin Cancer Res. 2018 Feb 15;24(4):794-806.  [Abstract]

    HSP90 inhibition with Luminespib or Ganetespib treatment at 50 and 100 nM for 24 hours in three CMS4 cell lines with response to HSP90 inhibition (CACO2, LIM2099 and SW480) confirmed up-regulation of HSP70 and HSP40 at the protein level in treated versus untreated control cells (western blotting).

    Luminespib purchased from MCE. Usage Cited in: Stem Cell Res. 2014 Sep;13(2):284-99.  [Abstract]

    HSP90 inhibition affects ciliation. 24 h treatment with 100 nM AUY922 significantly affects ciliation, under 20% (left) O2 tension but not 5% O2 tension (right).
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively[1].

    IC50 & Target[1]

    HSP90α

    7.8 nM (IC50)

    HSP90β

    21 nM (IC50)

    GRP94

    535 nM (IC50)

    TRAP-1

    85 nM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A2780 IC50
    0.001 μM
    Compound: NVP-AUY922
    Antiproliferative activity against human A2780 cells after 72 hrs
    Antiproliferative activity against human A2780 cells after 72 hrs
    [PMID: 24980703]
    A549 GI50
    0.01 μM
    Compound: 1; AUY-922
    Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay
    [PMID: 32683166]
    A549 GI50
    0.026 μM
    Compound: NVP-AUY922
    Growth inhibition of human A549 cells after 72 hrs by SRB assay
    Growth inhibition of human A549 cells after 72 hrs by SRB assay
    [PMID: 25313505]
    A549 IC50
    39 nM
    Compound: NVP-AUY922
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    [PMID: 32352777]
    A549 IC50
    60 nM
    Compound: AUY922
    Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
    Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
    [PMID: 29698859]
    BT-474 IC50
    0.01 μM
    Compound: NVP-AUY922
    Induction of Her2 degradation in human BT474 cells assessed as inhibition of signal by immunocytochemistry
    Induction of Her2 degradation in human BT474 cells assessed as inhibition of signal by immunocytochemistry
    [PMID: 24980703]
    BT-474 IC50
    14 nM
    Compound: AUY922
    Antiproliferative activity against human BT474 cells after 72 hrs by SRB assay
    Antiproliferative activity against human BT474 cells after 72 hrs by SRB assay
    [PMID: 29698859]
    CAPAN-1 IC50
    657 nM
    Compound: NVP-AUY922
    Antiproliferative activity against human Capan1 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    Antiproliferative activity against human Capan1 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    [PMID: 32352777]
    DU-145 GI50
    0.005 μM
    Compound: 40f, VER-52296, NVP-AUY922
    Growth inhibition of human DU145 cells by SRB assay
    Growth inhibition of human DU145 cells by SRB assay
    [PMID: 18020435]
    DU-145 IC50
    21 nM
    Compound: AUY922
    Antiproliferative activity against human DU145 cells after 72 hrs by SRB assay
    Antiproliferative activity against human DU145 cells after 72 hrs by SRB assay
    [PMID: 29698859]
    EBC-1 IC50
    13 nM
    Compound: AUY922
    Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay
    Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay
    [PMID: 29698859]
    Fibroblast CC50
    0.008 μM
    Compound: 2, AUY-922
    Cytotoxicity against Huntington's disease patient derived fibroblasts after 48 hrs by CellTiter Glo assay
    Cytotoxicity against Huntington's disease patient derived fibroblasts after 48 hrs by CellTiter Glo assay
    [PMID: 24673104]
    HCC827 IC50
    7 nM
    Compound: 7; NVP-AUY922
    Cytotoxicity against gefitinib-resistant human HCC827 cells assessed as inhibition of cell proliferation by MTS assay
    Cytotoxicity against gefitinib-resistant human HCC827 cells assessed as inhibition of cell proliferation by MTS assay
    [PMID: 26844689]
    HCT-116 GI50
    0.016 μM
    Compound: 40f, VER-52296, NVP-AUY922
    Growth inhibition of human HCT116 cells after 24 hrs by SRB assay
    Growth inhibition of human HCT116 cells after 24 hrs by SRB assay
    [PMID: 18020435]
    HCT-116 IC50
    121 nM
    Compound: NVP-AUY922
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    [PMID: 32352777]
    HCT-116 IC50
    16 nM
    Compound: AUY922
    Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
    [PMID: 29698859]
    L02 IC50
    1364 nM
    Compound: NVP-AUY922
    Cytotoxicity agains human HL7702 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    Cytotoxicity agains human HL7702 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    [PMID: 32352777]
    MDA-MB-231 IC50
    21 nM
    Compound: AUY922
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
    [PMID: 29698859]
    MIA PaCa-2 IC50
    38 nM
    Compound: NVP-AUY922
    Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    Antiproliferative activity against human MIAPaCa2 cells assessed as reduction in cell viability after 72 hrs by SRB assay
    [PMID: 32352777]
    NCI-H1975 GI50
    0.02 μM
    Compound: 1; AUY-922
    Antiproliferative activity against human NCI-H1975 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human NCI-H1975 cells measured after 48 hrs by SRB assay
    [PMID: 32683166]
    NCI-H3122 IC50
    0.014 μM
    Compound: 3; AUY922
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay
    [PMID: 27688186]
    NCI-H3122 IC50
    12.4 nM
    Compound: AUY922
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay
    [PMID: 29698859]
    NCI-H460 IC50
    0.0024 μM
    Compound: 5, NVP-AUY922
    Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 72 hrs by sulforhodamine B assay
    [PMID: 24565573]
    NCI-H460 IC50
    0.0024 μM
    Compound: 10, VER-52296/NVP-AUY922
    Cytotoxicity against human NCI-H460 after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human NCI-H460 after 72 hrs by sulforhodamine B assay
    [PMID: 22066525]
    NCI-H460 GI50
    0.03 μM
    Compound: 1; AUY-922
    Antiproliferative activity against human NCI-H460 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human NCI-H460 cells measured after 48 hrs by SRB assay
    [PMID: 32683166]
    NCI-H460 IC50
    2.4 nM
    Compound: NVP-AUY922
    Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 72 hrs by SRB assay
    Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 72 hrs by SRB assay
    [PMID: 24588105]
    NCI-H460 IC50
    23 nM
    Compound: AUY922
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by SRB assay
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by SRB assay
    [PMID: 29698859]
    NCI-N87 IC50
    83 nM
    Compound: AUY922
    Antiproliferative activity against human NCI-N87 cells after 72 hrs by SRB assay
    Antiproliferative activity against human NCI-N87 cells after 72 hrs by SRB assay
    [PMID: 29698859]
    PC-3M GI50
    0.006 μM
    Compound: 40f, VER-52296, NVP-AUY922
    Growth inhibition of human PC3M cells by SRB assay
    Growth inhibition of human PC3M cells by SRB assay
    [PMID: 18020435]
    SF-268 GI50
    0.006 μM
    Compound: 40f, VER-52296, NVP-AUY922
    Growth inhibition of human SF268 cells by SRB assay
    Growth inhibition of human SF268 cells by SRB assay
    [PMID: 18020435]
    Sf9 IC50
    8 nM
    Compound: NVP-AUY922
    Displacement of GM-BODIPY from human full length HSP90 alpha expressed in baculovirus-infected Sf9 cells after 16 hrs by fluorescence polarization assay
    Displacement of GM-BODIPY from human full length HSP90 alpha expressed in baculovirus-infected Sf9 cells after 16 hrs by fluorescence polarization assay
    [PMID: 24751441]
    SK-MEL-28 GI50
    0.005 μM
    Compound: 40f, VER-52296, NVP-AUY922
    Growth inhibition of human SKMel28 cells by SRB assay
    Growth inhibition of human SKMel28 cells by SRB assay
    [PMID: 18020435]
    U-87MG ATCC GI50
    0.008 μM
    Compound: 40f, VER-52296, NVP-AUY922
    Growth inhibition of human U87MG cells by SRB assay
    Growth inhibition of human U87MG cells by SRB assay
    [PMID: 18020435]
    U-87MG ATCC IC50
    31 nM
    Compound: AUY922
    Antiproliferative activity against human U87MG cells after 72 hrs by SRB assay
    Antiproliferative activity against human U87MG cells after 72 hrs by SRB assay
    [PMID: 29698859]
    体外研究
    (In Vitro)

    Luminespib 是一种强效且选择性的 HSP90 抑制剂,对 HSP90β 的 IC50s 值和 Kis 值分别为 21 ± 16、8.2 ± 0.7 nM,对 HSP90α 的 IC50s 值和 Kis 值分别为 7.8 ± 1.8、9.0 ± 5.0 nM。Luminespib 对 GRP94 和 TRAP-1 表现出较弱的活性,IC50s 值分别为 535 ± 51 nM(Ki,108 nM)和 85 ± 8 nM(Ki,53 nM)。 Luminespib 对各种人类肿瘤细胞系的增殖有抑制作用 (2.3-49.6 nM),诱导细胞周期停滞和凋亡,并消耗人类癌细胞中的客户蛋白 (80 nM)[1]。Luminespib (100 nM) 显著降低 CD40L 成纤维细胞诱导的免疫表型和 STAT3 信号传导变化,但对慢性淋巴细胞白血病 (CLL) 细胞的活力没有影响。Luminespib (500 nM) 与 NSC 118218 联合使用比单独使用任何一种药物更有效地诱导共培养细胞凋亡,并克服成纤维细胞对 Hsp90 抑制剂的耐药性[2]。Luminespib 对胰腺癌细胞表现出很强的抑制作用,IC50 值为 10 nM。 Luminespib (10 nM) 可降低 EGFR 的表达和表皮生长因子 (EGF) 介导的激活,并通过降低 ERKThr202/Tyr204 的下游磷酸化来显著破坏 EGF 信号传导。Luminespib (10 nM) 可在没有和存在 EGF 的情况下显著阻止胰腺癌细胞的迁移和侵袭[3]

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

    体内研究
    (In Vivo)

    Luminespib(50、75 mg/kg,腹腔注射)显著抑制肿瘤生长速度,降低人类肿瘤异种移植模型中第 11 天肿瘤的平均重量[2]
    Luminespib(50 mg/kg/周,3×25 mg/kg/周)显著降低 L3.6pl 胰腺癌细胞小鼠模型中的肿瘤生长速度并降低肿瘤重量[3]

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

    Clinical Trial
    分子量

    465.54

    Formula

    C26H31N3O5

    CAS 号
    性状

    固体

    颜色

    Light yellow to gray

    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
    细胞实验: 

    DMSO 中的溶解度 : ≥ 62 mg/mL (133.18 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 2.1480 mL 10.7402 mL 21.4804 mL
    5 mM 0.4296 mL 2.1480 mL 4.2961 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 year; -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

    动物实验:

    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.37 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。
    • 方案 二

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

      Solubility: ≥ 2.5 mg/mL (5.37 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      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。
    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: 99.81%

    参考文献
    Cell Assay
    [1]

    Cell lines are grown in DMEM/10% FCS, 2 mM glutamine, and nonessential amino acids in a humidified atmosphere of 5% CO2 in air. All lines are free of Mycoplasma. Cell proliferation is determined using the SRB assay for tumor cells and prostate epithelial cells, the WST-1 assay for MCF10A and HB119, or an alkaline phosphatase assay for HUVEC and HDMEC. GI50 is the compound concentration inhibiting cell proliferation by 50% compared with vehicle controls. Active caspase-3/7 is measured using a homogenous caspase assay kit[1].

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

    Animal Administration
    [1]

    Mice[1]
    For efficacy studies, human tumor xenografts are established s.c. in athymic mice. WM266.4 cells are also injected i.v. to generate experimental lung metastases and PC3LN3 prostate carcinoma cells are implanted into the prostates of male mice. Dosing by i.p. with Luminespib commences when tumors are well established. Tumor growth is monitored and at study end samples are harvested for analysis[1].

    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 year; -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 2.1480 mL 10.7402 mL 21.4804 mL 53.7011 mL
    5 mM 0.4296 mL 2.1480 mL 4.2961 mL 10.7402 mL
    10 mM 0.2148 mL 1.0740 mL 2.1480 mL 5.3701 mL
    15 mM 0.1432 mL 0.7160 mL 1.4320 mL 3.5801 mL
    20 mM 0.1074 mL 0.5370 mL 1.0740 mL 2.6851 mL
    25 mM 0.0859 mL 0.4296 mL 0.8592 mL 2.1480 mL
    30 mM 0.0716 mL 0.3580 mL 0.7160 mL 1.7900 mL
    40 mM 0.0537 mL 0.2685 mL 0.5370 mL 1.3425 mL
    50 mM 0.0430 mL 0.2148 mL 0.4296 mL 1.0740 mL
    60 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8950 mL
    80 mM 0.0269 mL 0.1343 mL 0.2685 mL 0.6713 mL
    100 mM 0.0215 mL 0.1074 mL 0.2148 mL 0.5370 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:
    Luminespib
    目录号:
    HY-10215
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