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ApexBio/AUY922 (NVP-AUY922)/10mM (in 1mL DMSO)/A4057
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AUY922 (NVP-AUY922)Potent Hsp90 inhibitor

Catalog No.A4057
SizePriceStockQty
10mM (in 1mL DMSO)
$75.00
In stock
5mg
$50.00
In stock
10mg
$70.00
In stock
25mg
$150.00
In stock
100mg
$350.00
In stock

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Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Product Citations

1.Jason E. Gestwicki, Co-Chair,et al. "Strategies and functional consequences of inhibiting protein-protein interactions." University of Michigan. 2016.

Related Compound Libraries

  • DiscoveryProbe™ Bioactive Compound Library
  • DiscoveryProbe™ Anti-cancer Compound Library
  • DiscoveryProbe™ Metabolism-related Compound Library

Quality Control

Quality Control & MSDS

View current batch:
    Purity = 98.26%
  • COA (Certificate Of Analysis)
  • HPLC (Retest)
  • NMR (Nuclear Magnetic Resonance)
  • MSDS (Material Safety Data Sheet)
  • Datasheet

Chemical structure

AUY922 (NVP-AUY922)

Related Biological Data

AUY922 (NVP-AUY922)

Related Biological Data

AUY922 (NVP-AUY922)

Related Biological Data

AUY922 (NVP-AUY922)

Biological Activity

DescriptionAUY922 (NVP-AUY922) is a highly potent inhibitor of HSP90 for HSP90α/β with IC50 of 13 nM /21 nM.
TargetsHSP90αHSP90β
IC5013 nM21 nM

Protocol

Cell experiment: [1]

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 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C 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 experiment : [2]

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.

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.

AUY922 (NVP-AUY922) Dilution Calculator

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Chemical Properties

Cas No. 747412-49-3SDF Download SDF
Synonyms VER-52296, AUY-922, AUY 922
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
Canonical SMILES CCNC(=O)C1=C(C(=C2C=C(C(=CC2=O)O)C(C)C)ON1)C3=CC=C(C=C3)CN4CCOCC4
Formula C26H31N3O5 M.Wt 465.5
Solubility ≥23.3 mg/mL in DMSO, ≥100.6 mg/mL in EtOH with ultrasonic, <2.57 mg/ml="" in="" h2o=""> Storage Store at -20°C
Physical AppearanceA solidShipping ConditionEvaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Research Update

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. Epub2013 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. Epub2013 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. Epub2013 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. Epub2013 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. Epub2012 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.

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.

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Western Blot 即免疫印迹试验,可以利用 Western Blot 来比较在不同条件下,不同细胞组织中目的蛋白表达量的差异,属于定 查看更多>
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最近做western越来越讨厌手上的这支内参gapdh。效价低不说,还最多只能用两次!条带也不够亮,还有背景。看到坛子里有人用1:10000还能回收好多次,不禁心生羡慕。故求助下哪家的内参抗体比较好?原装分装国产进口都可以。谢谢!~
很正常。内参有证明蛋白样品没问题。没有目的带原因很多。1.目的蛋白是否表达量很低,因为内参表达是很高的。2.抗体的选择是否有问题,有没有阳性对照?? 是一点都没有?还是能看到一点点?
高保真生物技术有限公司~实验整体外包服务商~
一抗多稀释点试试
我觉得封闭这一步时间长短多少并不能减少背景…背景过深多半还是抗体浓度过大…不管一抗还是二抗过大都会使背景加深…一抗的浓度不一定是条带清晰就是最佳了…联系进一步优化一下

这个主要还是抗体的问题,WB最主要的还是要选择一个特异性较好的抗体,抗体是整个实验的重中之重
内个,个人觉得比较价格还是很有说服力的,一分价钱一分货。
虽然没有具体用过检测这个抗原的抗体,但是如果希望抗体特异性好点,能检测丰度低的蛋白,还是选Abcam吧,Santa有时候全凭人品了,内参抗体什么的还能凑活,其他的比较勉强。
内个,个人觉得比较价格还是很有说服力的,一分价钱一分货。
虽然没有具体用过检测这个抗原的抗体,但是如果希望抗体特异性好点,能检测丰度低的蛋白,还是选Abcam吧,Santa有时候全凭人品了,内参抗体什么的还能凑活,其他的比较勉强。
Western Blot内参选择 123
逆枫军团_952017-09-28
内参bate-actin或GAPDH多为单抗,来源于小鼠,
一般可与大鼠、小鼠、人、兔均有交叉反应,即可作为上述任一来源蛋白的内参。
Actin分子量为42kD,为肌动蛋白
GAPDH分子量为36kD,为磷酸脱氢酶
内参蛋白的表达量一般比较大,而且内参蛋白的抗体通常比较好用。你要杂的目的蛋白可能表达量要远小于内参蛋白,又可能是目的蛋白的抗体不好用。因此可以考虑浓缩你的蛋白样品(增加细胞量、减少裂解液等方法)、增加目的蛋白抗体浓度、更换目的蛋白抗体。另外,化学发光试剂也可以换用更好的,比如GE公司的,虽然价格贵,但是灵敏度要比国产的试剂高出很多,希望能够帮到你。
actin
GAPDH
万能内参
主要看你的目标蛋白的分子量多大,“目标蛋白要与内参蛋白的分子量差异大!”
方便检测
核蛋白,有很多种,分子量不同
膜蛋白,有很多很多种,分子量不同
浆蛋白,有成千上万种,分子量不同。
具体实验,具体目的蛋白,具体的内参。
请教各位,我买的CST的beta-actin(#3700)抗体,说明书上的图片只有一条特异性条带(见图),为什么我做的实际情况是有很多杂带,我做的是脑组织蛋白,这个是怎么回事?
科研思路和方法作业123
若情初心2021-08-06
请教大鼠MCAO模型检测ZO-1免疫组化所用抗体,内参以及引物设计?
内参一般都会用β-actin, GAPDH
当然跟物种有关。

小鼠肝脏组织内参用小鼠来源的一抗二抗可以用山羊抗大鼠抗体吗?

如果是大鼠肝脏组织,可以用小鼠来源的一抗吗?

大鼠小鼠抗原抗体有区别吗?

求教,谢谢!

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