AUY922 (NVP-AUY922) (Synonyms: VER-52296, AUY-922, AUY 922, Luminespib) |
Catalog No.GC15295 |
An Hsp90 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 747412-49-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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) 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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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