AUY922 (NVP-AUY922) (Synonyms: VER-52296, AUY-922, AUY 922, Luminespib) |
| رقم الكتالوجGC15295 |
AUY922 (NVP-AUY922) is a potent and selective inhibitor of HSP90, effectively inhibiting both HSP90α and HSP90β with similar IC50 values of 13nM and 21nM, respectively.
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.
AUY922 (NVP-AUY922) is a potent and selective inhibitor of HSP90[1], effectively inhibiting both HSP90α and HSP90β with similar IC50 values of 13nM and 21nM, respectively[2]. AUY922 (NVP-AUY922) exhibits significant antitumor activity and is commonly utilized in the research of various cancers, including breast cancer, lung cancer[3], and gastrointestinal stromal tumors[4].
AUY922 (NVP-AUY922) inhibited the in vitro proliferation of human tumor cells, which selected for their different tissue origins and molecular features with nanomolar potency (2.3–49.6nmol/L) [5]. AUY922 (NVP-AUY922) (100, 500, 1000nM; 5, 15, 30, 60, 180min) treatment can induce HSP90-p23 dissociation and client protein depletion in a concentration and time dependent manner in BT-474 cells[6].
AUY922 (NVP-AUY922) (50, 75mg/kg) slowed growth of A549 (KRAS-mutant) xenografts and achieved tumor stability and decreased EGF receptor (EGFR) protein expression in H1975 xenografts model mice[7]. AUY922 (NVP-AUY922) (30mg/kg) combined with radiation treatment delayed tumor growth in a supra-additive manner in tumor xenograft model mice[8].
References:
[1]. Schilb A, Riou V, Schoepfer J, et al. Development and implementation of a highly miniaturized confocal 2D-FIDA-based high-throughput screening assay to search for active site modulators of the human heat shock protein 90beta. J Biomol Screen. 2004 Oct;9(7):569-77. doi: 10.1177/1087057104265538. PMID: 15475476.
[2]. Brough PA, Aherne W, Barril X, et al. 4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer. J Med Chem. 2008 Jan 24;51(2):196-218. doi: 10.1021/jm701018h. Epub 2007 Nov 20. PMID: 18020435.
[3]. Ueno T, Tsukuda K, Toyooka S, et al. Strong anti-tumor effect of NVP-AUY922, a novel Hsp90 inhibitor, on non-small cell lung cancer. Lung Cancer. 2012 Apr;76(1):26-31. doi: 10.1016/j.lungcan.2011.09.011. Epub 2011 Oct 11. PMID: 21996088.
[4]. Hsueh YS, Yen CC, Shih NY, et al. Autophagy is involved in endogenous and NVP-AUY922-induced KIT degradation in gastrointestinal stromal tumors. Autophagy. 2013 Feb 1;9(2):220-33. doi: 10.4161/auto.22802. Epub 2012 Nov 29. PMID: 23196876; PMCID: PMC3552885.
[5]. Eccles SA, Massey A, Raynaud FI, et al. NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis. Cancer Res. 2008 Apr 15;68(8):2850-60. doi: 10.1158/0008-5472.CAN-07-5256. PMID: 18413753.
[6]. Jensen MR, 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. doi: 10.1186/bcr1996. Epub 2008 Apr 22. PMID: 18430202; PMCID: PMC2397535.
[7]. Garon EB, Finn RS, Hamidi H, et al. 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. Epub 2013 Mar 14. PMID: 23493311; PMCID: PMC3681857.
[8]. Gandhi N, Wild AT, Chettiar ST, et al. Novel Hsp90 inhibitor NVP-AUY922 radiosensitizes prostate cancer cells. Cancer Biol Ther. 2013 Apr;14(4):347-56. doi: 10.4161/cbt.23626. Epub 2013 Jan 28. PMID: 23358469; PMCID: PMC3667875.
| Cell experiment [1]: | |
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Cell lines |
BT-474 cells |
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Preparation Method |
BT-474 cells were treated with AUY922 (NVP-AUY922) for different time. Then total cell extracts were prepared and the expression of HSP90 were analyzed by Western blot analysis. The amount of p23 associated with HSP90 was determined by immunoprecipitating p23 followed by immunoblotting for HSP90. |
|
Reaction Conditions |
100, 500, 1000nM; 5, 15, 30, 60, 180min |
|
Applications |
AUY922 (NVP-AUY922) induces HSP90-p23 dissociation and client protein depletion in a concentration- and time dependent manner. |
| Animal experiment [2]: | |
|
Animal models |
Non–Small Cell Lung cancer xenograft mouse model |
|
Preparation Method |
Mice carrying subcutaneous A549 xenograft tumors were treated with 25 to 75 mg/kg AUY922 (NVP-AUY922). Then the tumor volume were measured manually with calipers at the indicated time. |
|
Dosage form |
25, 50, 75mg/kg; weekly,5 weeks; i.v. |
|
Applications |
AUY922 (NVP-AUY922) treatment can reduce tumor growth rates in xenograft models in a dose-dependent manner. |
|
References: |
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| Cas No. | 747412-49-3 | SDF | |
| المرادفات | 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 |
| الذوبان | ≥ 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1482 mL | 10.7411 mL | 21.4823 mL |
| 5 mM | 429.6 μL | 2.1482 mL | 4.2965 mL |
| 10 mM | 214.8 μL | 1.0741 mL | 2.1482 mL |
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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