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AUY922(NVP-AUY922)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AUY922(NVP-AUY922)图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
100mg电议

产品介绍
AUY922 (NVP-AUY922) (VER-52296) 是一种有效的 HSP90 抑制剂,对 HSP90α 的 IC50 分别为 7.8 和 21 nM;和 HSP90β;分别。

Cell lines

NCI-N87, SNU-216 and SNU-484 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Reaction Conditions

200 nM, 24 h

Applications

AUY922 reduced expression of client proteins. It decreased expression of receptor tyrosine kinases, such as VEGFR1, 2, 3 and PDGFR-α. It also decreased Akt and phospho-Akt in a dose-dependent manner. Besides that, AUY922 treatment resulted in decreased expression of HER-2 in NCI-N87 cells.

Animal models

Athymic Nude-nu mice injected with BT-474 breast cancer xenograft

Dosage form

Intravenous acute administration, 30 mg/kg

Applications

A significant effect of AUY922 on HSP90-p23 complex dissociation was observed at the 2- and 6-hour time points. From 16 and 24 hours after compound administration, HSP90-p23 complexes reassembled in the BT-474 xenografts. AUY922 also induced phospho-AKT level reduction.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

AUY922 (NVP-AUY922) is a potent, novel synthetic resorcinylic isoxazole amide inhibitor of heat shock protein 90 (HSP90).[1]It is a small molecular with the formula of C26H31N3O5and molecular weight of 465.5. It has a much higher affinity for Hsp90 and can be ound to the ATP binding site of Hsp90 at the N-terminal domain.[2]Heat shock protein 90 (HSP90) is a molecular chaperone essential for the stability of key regulators of cell growth and survival. NVP-AUY922 potently inhibits the proliferation of gastric cancer cell lines with with GI50 values of approximately 2 to 40 nmol/L and significantly induces the degradation of growth factor receptors and other client proteins.[3]

References:

[1]Suzanne A. E, Andy M, Florence I. R, et al. NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis. Cancer Res. 2008, 68. 2850-2860.

[2] Tsuyoshi U, Kazunori T, Shinichi T, Midori A, Munenori T, et al. Strong anti-tumor effect of NVP-AUY922, a novel Hsp90 inhibitor, on non-small cell lung cancer. Lung Cancer. 2012, 76. 26-31.

[3] Kyung-Hun L, Ju-Hee L, Sae-Won H, Seock-Ah I, 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, 102. 1388–1395.