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Luminespib

产品编号 T1989 CAS 747412-49-3

别名: AUY922, VER-52296, NVP-AUY922

Luminespib (VER-52296) 是一种 HSP90抑制剂，抑制 HSP90α 和 HSP90β 的 IC50分别为 7.8 和 21 nM。

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Luminespib, CAS 747412-49-3

规格	价格/CNY	货期
1 mg	￥ 186	现货
5 mg	￥ 398	现货
10 mg	￥ 573	现货
25 mg	￥ 1,230	现货
50 mg	￥ 1,880	现货
100 mg	￥ 2,890	现货
200 mg	￥ 4,270	现货
500 mg	￥ 6,830	现货
1 mL * 10 mM (in DMSO)	￥ 443	现货

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其他形式的 Luminespib:

Luminespib mesylate
询价

选择批次

纯度: 99.25%

纯度: 98.97%

纯度: 98%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Luminespib (VER-52296) is a new-type inhibitor of HSP90 (IC50s: 7.8/21 nM for HSP90α/β in cell free assay).
靶点活性	HSP90 β:21 nM (cell free), HSP90 α:7.8 nM (cell free)
体外活性	Luminespib (NVP-AUY922) potently inhibits HSP90 (Kd = 1.7 nmol/L) and proliferation of human tumor cells with GI50 values of approximately 2 to 40 nmol/L, inducing G(1)-G(2) arrest and apoptosis [1]. In 11 human gastric cancer cell lines, The IC50 values of NVP-AUY922 fell in the nanomolar range of 2–40 nM. The IC50 values for the cell lines NCI-N87 and SNU-216, cells with HER-2 amplification, were 3.23 nM and 11.99 nM, respectively [2]. NVP-AUY922 inhibited the proliferation of oral squamous cell carcinoma cells in vitro. NVP-AUY922 caused degradation of client protein inducing ErbB2, p-Akt, p-S6, HIF1-α and VEGF and up-regulation of HSP70 in HSC-2 oral squamous cell carcinoma [3].
体内活性	Daily dosing of NVP-AUY922 (50 mg/kg i.p. or i.v.) to athymic mice generated peak tumor levels at least 100-fold above cellular GI(50). This produced statistically significant growth inhibition and/or regressions in human tumor xenografts with diverse oncogenic profiles: BT474 breast tumor treated/control, 21%; A2780 ovarian, 11%; U87MG glioblastoma, 7%; PC3 prostate, 37%; and WM266.4 melanoma, 31% [1]. Luminespib was administered at 50 mg/kg daily i.p. to athymic mice bearing HCT116 human colon carcinoma xenografts. The rate of tumor growth was significantly inhibited by Luminespib administration, and treated tumor weights measured at day 12 were 49.8% of the control values [4].
细胞实验	Cell lines were grown in DMEM/10% FCS, 2 mmol/L glutamine, and nonessential amino acids in a humidified atmosphere of 5% CO2 in air. All lines were free of Mycoplasma. Cell proliferation was determined using the sulforhodamine B (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 was the compound concentration inhibiting cell proliferation by 50% compared with vehicle controls. Cell cycle analysis was as described. Active caspase-3/7 was measured using a homogenous caspase assay kit [1].
动物实验	In vivo, pharmacokinetic studies in female NCr athymic mice bearing WM266.4 human melanoma xenografts were essentially as described. NVP-AUY922 was dissolved in DMSO and diluted in sterile saline/Tween 20. A single dose of 50 mg/kg NVP-AUY922 was given i.v. or i.p. and groups of three animals were taken at intervals for pharmacokinetic analyses [1].

别名	AUY922, VER-52296, NVP-AUY922
分子量	465.54
分子式	C26H31N3O5
CAS No.	747412-49-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 86 mg/mL (184.7 mM)

Ethanol: 29 mg/mL (62.3 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	2.148 mL	10.7402 mL	21.4804 mL	53.7011 mL
	5 mM	0.4296 mL	2.148 mL	4.2961 mL	10.7402 mL
	10 mM	0.2148 mL	1.074 mL	2.148 mL	5.3701 mL
	20 mM	0.1074 mL	0.537 mL	1.074 mL	2.6851 mL
	50 mM	0.043 mL	0.2148 mL	0.4296 mL	1.074 mL
DMSO	100 mM	0.0215 mL	0.1074 mL	0.2148 mL	0.537 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Eccles, Suzanne A., et al. NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis. Cancer Research (2008), 68(8), 2850-2860. 2. Lee KH, et al. Antitumor activity of NVP-AUY922, a novel heat shock protein 90 inhibitor, in human gastric cancer cells is mediated through proteasomal degradation of client proteins. Cancer Sci. 2011 Jul;102(7):1388-95. 3. Okui T, et al. Antitumor effect of novel HSP90 inhibitor NVP-AUY922 against oral squamous cell carcinoma. Anticancer Res. 2011 Apr;31(4):1197-204. 4. Brough PA, et al. 4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. J Med Chem. 2008 Jan 24;51(2):196-218. 5. Han H W, Hahn S, Jeong H Y, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent[J]. Scientific reports. 2018 Oct 8;8(1):14969. 6. Wang Y, Ma H, Huang J, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors[J]. European Journal of Medicinal Chemistry. 2020: 113030.

文献引用

1. He C X, Lv Y, Guo M, et al. Complex Crystal Structure Determination of Hsp90 N-NVP-AUY922 and In Vitro Anti-NSCLC Activity of NVP-AUY922. Frontiers in oncology. 2022, 12: 847556-847556. 2. He C X, Lv Y, Guo M, et al. Complex Crystal Structure Determination of Hsp90N-NVP-AUY922 and In Vitro Anti-NSCLC Activity of NVP-AUY922. Frontiers in oncology. 2022, 12 3. Wang Y, Ma H, Huang J, et al. Discovery of bardoxolone derivatives as novel orally active necroptosis inhibitors. European Journal of Medicinal Chemistry,. 2021 Feb 15;212:113030 4. Han H W, Hahn S, Jeong H Y, et al. LINCS L1000 dataset-based repositioning of CGP-60474 as a highly potent anti-endotoxemic agent. Scientific Reports. 2018 Oct 8;8(1):14969 5. Li J, Han X, Sun M, et al.Caspase-9 inhibition triggers Hsp90-based chemotherapy-mediated tumor intrinsic innate sensing and enhances antitumor immunity.Journal for Immunotherapy of Cancer.2023, 11(12).

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Luminespib 747412-49-3 Apoptosis Autophagy Cytoskeletal Signaling Metabolism HSP VER 52296 AUY922 VER-52296 Inhibitor AUY-922 Heat shock proteins VER52296 AUY 922 inhibit NVP-AUY922 NVP-AUY 922 NVP-AUY-922 inhibitor

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Luminespib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords