| AUY922 (NVP-AUY922) Potent Hsp90 inhibitor |
Sample solution is provided at 25 µL, 10mM.
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Chemical structure
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Related Biological Data
| Description | AUY922 (NVP-AUY922) is a highly potent inhibitor of HSP90 for HSP90α/β with IC50 of 13 nM /21 nM. | |||||
| Targets | HSP90α | HSP90β | ||||
| IC50 | 13 nM | 21 nM | ||||
| Cell experiment: [1] | |
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Cell lines |
NCI-N87, SNU-216 and SNU-484 cells |
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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. |
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Reaction Conditions |
200 nM, 24 h |
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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] | |
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Animal models |
Athymic Nude-nu mice injected with BT-474 breast cancer xenograft |
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Dosage form |
Intravenous acute administration, 30 mg/kg |
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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. |
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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. |
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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
AUY922 (NVP-AUY922) Molarity Calculator
| Cas No. | 747412-49-3 | SDF | 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 | ≥23.3mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request | ||
| General tips | For 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. | ||
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.
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.
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.
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.
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.
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.