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Luminespib

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。

CAS号

747412-49-3

分子式

C26H31N3O5

主要靶点

Apoptosis|Autophagy|HSP

仅限科研使用

Cat No : CM04651

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Synonyms

VER-52296|AUY922|NVP-AUY922

验证数据展示

  • CAS No.: 747412-49-3

    Luminespib
    CAS#: 747412-49-3

产品信息

AUY922 (NVP-AUY922) is a new-type inhibitor of HSP90 (IC50s: 7.8/21 nM for HSP90α/β in cell free assay).

CAS号 747412-49-3
分子式 C26H31N3O5
主要靶点 Apoptosis|Autophagy|HSP
主要通路 代谢|自噬|凋亡|细胞骨架
分子量 465.54
纯度 99.25%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 VER-52296|AUY922|NVP-AUY922

靶点活性

HSP90β:21 nM (cell free)|HSP90α:7.8 nM (cell free)

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].

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].

溶解度

Ethanol:29 mg/mL (62.3 mM),DMSO:86 mg/mL (184.7 mM),H2O:<1 mg/mL

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].

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.

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