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AUY922 (NVP-AUY922)Hsp90抑制剂

AUY922 (NVP-AUY922)

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10mM (in 1mL DMSO) ¥750.00 现货
5mg ¥500.00 现货
10mg ¥700.00 现货
25mg ¥1,500.00 现货
100mg ¥3,500.00 现货

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Sample solution is provided at 25 µL, 10mM.

引用文献

质量控制

化学结构

AUY922 (NVP-AUY922)

相关生物数据

AUY922 (NVP-AUY922)

相关生物数据

AUY922 (NVP-AUY922)

相关生物数据

AUY922 (NVP-AUY922)

AUY922 (NVP-AUY922) Dilution Calculator

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AUY922 (NVP-AUY922) Molarity Calculator

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化学性质

CAS号 747412-49-3 SDF Download SDF
别名 VER-52296, AUY-922, AUY 922
化学名 (5Z)-N-ethyl-5-(4-hydroxy-6-oxo-3-propan-2-ylcyclohexa-2,4-dien-1-ylidene)-4-[4-(morpholin-4-ylmethyl)phenyl]-2H-1,2-oxazole-3-carboxamide
SMILES CCNC(=O)C1=C(C(=C2C=C(C(=CC2=O)O)C(C)C)ON1)C3=CC=C(C=C3)CN4CCOCC4
分子式 C26H31N3O5 分子量 465.5
溶解度 ≥23.3 mg/mL in DMSO, ≥100.6 mg/mL in EtOH with ultrasonic, <2.57 mg/mL in H2O 储存条件 Store at -20°C
物理性状 A solid 运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

描述 AUY922 (NVP-AUY922)是一种高效的HSP90抑制剂,作用于HSP90α/β,IC50值为13 nM /21 nM。
靶点 HSP90α HSP90β        
IC50 13 nM 21 nM        

实验操作

细胞实验[1]:

细胞系

NCI-N87、SNU-216和SNU-484细胞

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

200 nM;24 h

应用

AUY922减少客户蛋白的表达,减少受体酪氨酸激酶的表达,比如VEGFR1、2、3和PDGFR-α,以剂量依赖的方式减少Akt和磷酸化Akt。除此之外,在NCI-N87细胞中,AUY922减少HER-2的表达。

动物实验[2]:

动物模型

BT-474乳腺癌异种移植无胸腺Nude-nu裸鼠

剂量

30 mg/kg;静脉给药

应用

在2和6小时的时间点观察到AUY922对HSP90-p23复合体解离的显著效应。在BT-474异种移植模型中,AUY922处理后的16和24小时观察到HSP90-p23复合体的重新装配,AUY922也诱导磷酸化AKT水平的下降。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Lee K H, Lee J H, Han S W, 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 science, 2011, 102(7): 1388-1395.

[2] Jensen M R, Schoepfer J, Radimerski T, et al. NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models. Breast Cancer Res, 2008, 10(2): R33.

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研究更新

1. Inhibition of HSP90 with AUY922 induces synergy in HER2-amplified trastuzumab-resistant breast and gastric cancer. Mol Cancer Ther. 2013 Apr;12(4):509-19. doi: 10.1158/1535-7163.MCT-12-0507. Epub 2013 Feb 8.
Abstract
The mono-therapy of AUY922 in the low nanomolar range potently inhibited proliferation of human gastric and breast cancer cells exhibiting a greater sensitivity to HER2-amplified cells than HER2-negative cells; while the combination of AUY922 and trastuzumab showed synergistic anticancer effect in conditioned trastuzumab-resistant models.
2. Novel Hsp90 inhibitor NVP-AUY922 radiosensitizes prostate cancer cells. Cancer Biol Ther. 2013 Apr;14(4):347-56. doi: 10.4161/cbt.23626. Epub 2013 Jan 28.
Abstract
AUY922 greatly increased the sensitivity of prostate cancer cells, Myc-CaP and PC3, to radiation and worked synergistically with radiation to increase apoptotic cell death, induce G2-M arrest, affect client protein expression and delay tumor growth.
3. The HSP90 inhibitor NVP-AUY922 potently inhibits non-small cell lung cancer growth. Mol Cancer Ther. 2013 Jun;12(6):890-900. doi: 10.1158/1535-7163.MCT-12-0998. Epub 2013 Mar 14.
Abstract
AUY922 ont only exhibited potent anticancer activity against NSCLC cells with IC50 and IC100 of 100 and 40 nmol/L respectively but also affected expression of genes involved in various cellular functions including decreased dihydrofolate reductase, where exposure to AUY922 stably slowed growth of A549 xenografts and decreased the expression of EGFR protein in H1975 xenografts.
4. The HSP90 inhibitor NVP-AUY922-AG inhibits the PI3K and IKK signalling pathways and synergizes with cytarabine in acute myeloid leukaemia cells. Br J Haematol. 2013 Apr;161(1):57-67. doi: 10.1111/bjh.12215. Epub 2013 Jan 29.
Abstract
NVP-AUY922-AG alone or synergistically with Ara-C exhibited anti-cancer activity against myeloid cell lines and primary AML blasts with significantly less toxicity to normal bone marrow, in which it induced increases in HSP70 expression and depletion of total AKT, IKKα and IKKβ.
5. Antiproliferative effect of the HSP90 inhibitor NVP-AUY922 is determined by the expression of PTEN in esophageal cancer. Oncol Rep. 2013 Jan;29(1):45-50. doi: 10.3892/or.2012.2074. Epub 2012 Oct 9.
Abstract
NVP-AUY922 significantly suppressed the activity of AKT and ERK and potently induced antiproliferation in ESCC cells, which are negatively associated with PETN expression.

产品描述

AUY922(NVP-AUY922)是一种有效的、新合成的间苯二酚异恶唑酰胺(resorcinylic isoxazole amide)类热休克蛋白90(HSP90,heat shock protein 90)的小分子抑制剂,分子式为C26H31N3O5,分子量为465.5,对Hsp90有高亲和性,可以与Hsp90 N端结构域的ATP结合位点相结合[1][2]。HSP90是一种分子伴侣,对调节细胞生长和存活的关键蛋白的稳定性是至关重要的。NVP-AUY922可以有效抑制胃癌细胞的增殖,GI50值约为2-40 nmol/L,也可以显著诱导生长因子受体和其它目标蛋白的降解[3]。

参考文献:
[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.