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: 99.89%
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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10 mM * 1 mL in DMSO ¥660
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10 mg ¥800
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25 mg ¥1500
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500 mg ¥11000
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Top Publications Citing Use of Products

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

    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.

    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).

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

    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.
    • 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

    HSP90α

    7.8 nM (IC50)

    HSP90β

    21 nM (IC50)

    GRP94

    535 nM (IC50)

    TRAP-1

    85 nM (IC50)

    体外研究
    (In Vitro)

    Luminespib is a potent and selective HSP90 inhibitor, with IC50s and Kis of 21 ± 16, 8.2 ± 0.7 nM against HSP90β and of 7.8 ± 1.8, 9.0 ± 5.0 nM for HSP90α. Luminespib shows weak activity against GRP94 and TRAP-1 wich IC50s of 535 ± 51 nM (Ki, 108 nM) and 85 ± 8 nM (Ki, 53 nM), respectively. Luminespib exhibits inhibitory effect on proliferation of various human tumor cell lines (2.3-49.6 nM), induces cell cycle arrest and apoptosis and depletes client proteins in human cancer cells (80 nM)[1]. Luminespib (100 nM) significantly reduces CD40L fibroblast-induced changes in immunophenotype and STAT3 signaling but with no effect on the viability of chronic lymphocytic leukemia (CLL) cells. Luminespib (500 nM) in combination with NSC 118218 more effectively induces apoptosis in cells in co-culture than either drug alone, and overcomes fibroblast-derived resistance to Hsp90 inhibitor[2]. Luminespib shows great inhibition of pancreatic cancer cells with IC50 of at 10 nM. Luminespib (10 nM) reduces the expression and the epidermal growth factor (EGF)-mediated activation of EGFR and substantially disrupts EGF signaling in terms of diminishing downstream phosphorylation of ERKThr202/Tyr204. Luminespib (10 nM) significantly blocks pancreatic cancer cell migration and invasion both in the absence and presence of EGF[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, i.p.) significantly inhibits tumor growth rate, reducing the mean weights of tumors on day 11 in human tumor xenografts[2]. Luminespib (50 mg/kg/week, 3×25 mg/kg/week) significantly reduces tumor growth rates and lowers tumor weights in the L3.6pl pancreatic cancer cell-bearing mice model[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
    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 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : ≥ 62 mg/mL (133.18 mM)

    * "≥" 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
    10 mM 0.2148 mL 1.0740 mL 2.1480 mL
    *

    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。-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。

    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

    • 1.

      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); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.37 mM,饱和度未知) 的澄清溶液。

      以 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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 2.

      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); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.37 mM,饱和度未知) 的澄清溶液。

      以 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。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.37 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 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玉米油中,混合均匀。

    • 4.

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

    • 5.

      请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

    *以上所有助溶剂都可在 MCE 网站选购。
    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

    纯度: 99.89%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

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

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    Luminespib
    目录号:
    HY-10215
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