Home>>Signaling Pathways>> Ubiquitination/ Proteasome>> Autophagy>>AUY922 (NVP-AUY922)

AUY922 (NVP-AUY922) (Synonyms: VER-52296, AUY-922, AUY 922, Luminespib)

Catalog No.GC15295

An Hsp90 inhibitor

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AUY922 (NVP-AUY922) Chemical Structure

Cas No.: 747412-49-3

Size Price Stock Qty
10mM (in 1mL DMSO)
$54.00
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5mg
$36.00
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10mg
$54.00
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25mg
$112.00
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100mg
$262.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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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.

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.

Chemical Properties

Cas No. 747412-49-3 SDF
Synonyms VER-52296, AUY-922, AUY 922, Luminespib
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°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.1482 mL 10.7411 mL 21.4823 mL
5 mM 0.4296 mL 2.1482 mL 4.2965 mL
10 mM 0.2148 mL 1.0741 mL 2.1482 mL
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