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ApexBio/AUY922 (NVP-AUY922)/10mM (in 1mL DMSO)/A4057
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.product-side h2 span {width: 50%;}.product-side h2 span.hover {}Related ProductsXL-888NVP-BEP800BIIB021RetaspimycinPF-04929113 (SNX-5422)IPI-504 (Retaspimycin hydrochloride)Molarity CalculatorDilution Calculator AUY922 (NVP-AUY922)Potent Hsp90 inhibitorCatalog No.A4057SizePriceStockQty10mM (in 1mL DMSO)$75.00In stock 5mg$50.00In stock 10mg$70.00In stock 25mg$150.00In stock 100mg$350.00In stock Tel: +1-832-696-8203Email: sales@apexbt.comWorldwide Distributors Add to CartBulk InquiryFree samples Check OutSample solution is provided at 25 µL, 10mM.Product Citations1.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 LibraryDiscoveryProbe™ Anti-cancer Compound LibraryDiscoveryProbe™ Metabolism-related Compound LibraryQuality Control Quality Control & MSDS View current batch: 21 Purity = 97.87% COA (Certificate Of Analysis) HPLC NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Purity = 98.26% COA (Certificate Of Analysis) HPLC (Retest) NMR (Nuclear Magnetic Resonance) MSDS (Material Safety Data Sheet) Datasheet Chemical structure Related Biological Data Related Biological Data Related Biological Data Biological ActivityDescriptionAUY922 (NVP-AUY922) is a highly potent inhibitor of HSP90 for HSP90α/β with IC50 of 13 nM /21 nM.TargetsHSP90αHSP90βIC5013 nM21 nMProtocolCell experiment: [1]Cell linesNCI-N87, SNU-216 and SNU-484 cellsPreparation methodThe 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 Conditions200 nM, 24 hApplicationsAUY922 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 modelsAthymic Nude-nu mice injected with BT-474 breast cancer xenograftDosage formIntravenous acute administration, 30 mg/kgApplicationsA 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 notesPlease 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 CalculatorConcentration (start)xVolume (start)=Concentration (final)xVolume (final) femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter femtomolar picomolar nanomolar micromolar millimolar molar microliter milliliter liter C1V1C2V2calculateAUY922 (NVP-AUY922) Molarity CalculatorMass=ConcentrationxVolumexMW* picograms nanograms micrograms milligrams grams kilograms femtomolar picomolar nanomolar micromolar millimolar molar nanoliter microliter milliliter liter g/molcalculate 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, Storage Store at -20°CPhysical AppearanceA solidShipping ConditionEvaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon requestGeneral 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.BackgroundAUY922 (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.

APExBIO(APExBIO Technology LLC)总部位于美国休斯顿,是一家自主研发生产、致力于为生命科学研究提供高性能产品和优质服务的供应商。公司现阶段涵盖丰富的产品线,主要包括:1. 10000 多种小分子抑制剂/激动剂——用于肿瘤、免疫、神经等生物医药各研究领域。2. 40 余个高通量化合物库——药物筛选最佳工具。3. 分子生物学产品——PCR、逆转录、qPCR、克隆、高通量 DNA 文库构建等试剂和试剂盒,公司对相关酶进行改造,使其稳定性、催化活性等有极大的提升。4. 体外转录——公司拥有国内独家mRNA体外转录合成平台,提供优质的修饰核苷酸、转录酶等各种合成原料,并可提供mRNA订制服务。5. Cy 染料、生物素——高纯度、种类丰富的 Cy 染料和生物素可用于蛋白检测、纯化等研究。6. 免疫学产品——各类细胞器染料及靶标信号放大的链霉亲和素系列和TSA系列。7. 试剂盒——高性能的 MTT、CCK-8、EdU 细胞增殖与毒性检测 Kit 和 Annexin V、Caspase 凋亡检测 Kit。8. 蛋白研究——蛋白提取抑制剂 cocktail、磷酸化蛋白研究新工具 phosbind。9. 组学服务——提供微生物多样性、转录组学等高通量测序服务。

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