NVP-AUY922

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NVP-AUY922
NVP-AUY 922.svg
Identifiers
CAS number 747412-49-3 N
ChemSpider 21377936 YesY
ChEMBL CHEMBL252164 YesY
Jmol-3D images Image 1
Properties
Molecular formula C26H31N3O5
Molar mass 465.54 g mol−1
Appearance Colorless solid[1]
Except where noted otherwise, data are given for materials in their standard state (at 25 °C (77 °F), 100 kPa)
 N (verify) (what is: YesY/N?)
Infobox references

NVP-AUY922 is an experimental drug candidate for the treatment of cancer. It was discovered through a collaboration between The Institute of Cancer Research and the pharmaceutical company Vernalis[2] and licensed to Novartis.[3] It is currently in Phase II clinical trials.[4]

NVP-AUY922 is an inhibitor of heat shock protein 90 (Hsp90),[1] which is a chaperone protein that plays a role in the modification of a variety of proteins that have been implicated in oncogenesis. NVP-AUY922 has shown promising activity in preclinical testing against several different tumor types.[5][6][7][8]

See also[edit]

References[edit]

  1. ^ a b Brough, Paul A.; Aherne, Wynne; Barril, Xavier; Borgognoni, Jenifer; Boxall, Kathy; Cansfield, Julie E.; Cheung, Kwai-Ming J.; Collins, Ian; Davies, Nicholas G. M. (2008). "4,5-Diarylisoxazole Hsp90 Chaperone Inhibitors: Potential Therapeutic Agents for the Treatment of Cancer". Journal of Medicinal Chemistry 51 (2): 196–218. doi:10.1021/jm701018h. PMID 18020435. 
  2. ^ "Structure-based design of cancer therapeutics". The Institute of Cancer Research. 
  3. ^ "AUY922". Vernalis. 
  4. ^ "Small caps: Vernalis drug fillip". Financial Times. July 19, 2011. 
  5. ^ Jensen, Michael; Schoepfer, Joseph; Radimerski, Thomas; Massey, Andrew; Guy, Chantale T; Brueggen, Josef; Quadt, Cornelia; Buckler, Alan; Cozens, Robert (2008). "NVP-AUY922: a small molecule HSP90 inhibitor with potent antitumor activity in preclinical breast cancer models". Breast Cancer Research 10 (2): R33. doi:10.1186/bcr1996. PMC 2397535. PMID 18430202. 
  6. ^ Gaspar, N.; Sharp, S. Y.; Eccles, S. A.; Gowan, S.; Popov, S.; Jones, C.; Pearson, A.; Vassal, G.; Workman, P. (2010). "Mechanistic Evaluation of the Novel HSP90 Inhibitor NVP-AUY922 in Adult and Pediatric Glioblastoma". Molecular Cancer Therapeutics 9 (5): 1219–1233. doi:10.1158/1535-7163.MCT-09-0683. PMC 2875164. PMID 20457619. 
  7. ^ Okui, T; Shimo, T; Hassan, NM; Fukazawa, T; Kurio, N; Takaoka, M; Naomoto, Y; Sasaki, A (2011). "Antitumor effect of novel HSP90 inhibitor NVP-AUY922 against oral squamous cell carcinoma". Anticancer research 31 (4): 1197–204. PMID 21508365. 
  8. ^ Eccles, S. A.; Massey, A.; Raynaud, F. I.; Sharp, S. Y.; Box, G.; Valenti, M.; Patterson, L.; De Haven Brandon, A.; Gowan, S. (2008). "NVP-AUY922: A Novel Heat Shock Protein 90 Inhibitor Active against Xenograft Tumor Growth, Angiogenesis, and Metastasis". Cancer Research 68 (8): 2850–2860. doi:10.1158/0008-5472.CAN-07-5256. PMID 18413753.