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AUY922 (NVP-AUY922)

现货
Catalog No.
A4057
Hsp90抑制剂
组合的产品项目
规格价格库存 数量
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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Background

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 C26H31N3O5 and 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.

文献引用

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt465.5
Cas No.747412-49-3
FormulaC26H31N3O5
SynonymsVER-52296, AUY-922, AUY 922
Solubility≥23.3 mg/mL in DMSO, ≥100.6 mg/mL in EtOH with ultrasonic, <2.57 mg/mL in H2O
Chemical Name(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
SDFDownload SDF
Canonical SMILESCCNC(=O)C1=C(C(=C2C=C(C(=CC2=O)O)C(C)C)ON1)C3=CC=C(C=C3)CN4CCOCC4
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。

试验操作

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.

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        

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)