NVP-AUY922

• CAT Number: I004773
• CAS Number: 747412-49-3
• Molecular Formula: C₂₆H₃₁N₃O₆
• Molecular Weight: 465.54
• Purity: ≥95%
• Target: HSP
• Solubility: DMSO: ≥ 62 mg/mL
• Storage: 3 years -20℃ powder
• IC50: 13 nM(HSP90α); 21 nM(HSP90β)
• IUPAC Name: 5-(2,4-dihydroxy-5-propan-2-ylphenyl)-N-ethyl-4-[4-(morpholin-4-ylmethyl)phenyl]-1,2-oxazole-3-carboxamide
• InChI: InChI=1S/C26H31N3O5/c1-4-27-26(32)24-23(18-7-5-17(6-8-18)15-29-9-11-33-12-10-29)25(34-28-24)20-13-19(16(2)3)21(30)14-22(20)31/h5-8,13-14,16,28,30H,4,9-12,15H2,1-3H3,(H,27,32)/b25-20-
• InChIKey: SWDZPNJZKUGIIH-QQTULTPQSA-N
• SMILES: CCNC(=O)C1=C(C(=C2C=C(C(=CC2=O)O)C(C)C)ON1)C3=CC=C(C=C3)CN4CCOCC4

NVP-AUY922 (Cat.No:I004773) is a small molecule inhibitor of heat shock protein 90 (Hsp90), a chaperone protein involved in cancer cell survival and proliferation. As a potent Hsp90 inhibitor, NVP-AUY922 has shown promising anticancer activity in preclinical studies, particularly against solid tumors. Clinical trials are ongoing to evaluate its efficacy and safety as a potential cancer therapy.

Reference

1:NVP-AUY922, a novel HSP90 inhibitor, inhibits the progression of malignant pheochromocytoma in vitro and in vivo. Lian J, Lin D, Xie X, Xu Y, Xu L, Meng L, Zhu Y.Onco Targets Ther. 2017 Apr 19;10:2219-2226. doi: 10.2147/OTT.S130236. eCollection 2017. PMID: 28458565 Free PMC Article2:HSP90 inhibitor NVP-AUY922 induces cell apoptosis by disruption of the survivin in papillary thyroid carcinoma cells. Liu J, Sun W, Dong W, Wang Z, Qin Y, Zhang T, Zhang H.Biochem Biophys Res Commun. 2017 May 27;487(2):313-319. doi: 10.1016/j.bbrc.2017.04.056. Epub 2017 Apr 13. PMID: 28412368 3:Dual PI3K- and mTOR-inhibitor PI-103 can either enhance or reduce the radiosensitizing effect of the Hsp90 inhibitor NVP-AUY922 in tumor cells: The role of drug-irradiation schedule. Djuzenova CS, Fiedler V, Katzer A, Michel K, Deckert S, Zimmermann H, Sukhorukov VL, Flentje M.Oncotarget. 2016 Jun 21;7(25):38191-38209. doi: 10.18632/oncotarget.9501. PMID: 27224913 Free PMC Article4:2-phenylethynesulphonamide (PFT-μ) enhances the anticancer effect of the novel hsp90 inhibitor NVP-AUY922 in melanoma, by reducing GSH levels. Yeramian A, Vea A, Benítez S, Ribera J, Domingo M, Santacana M, Martinez M, Maiques O, Valls J, Dolcet X, Vilella R, Cabiscol E, Matias-Guiu X, Marti RM.Pigment Cell Melanoma Res. 2016 May;29(3):352-71. doi: 10.1111/pcmr.12472. PMID: 26988132 5:The novel HSP90 inhibitor NVP-AUY922 shows synergistic anti-leukemic activity with cytarabine in vivo. Wendel T, Zhen Y, Suo Z, Bruheim S, Wiedlocha A.Exp Cell Res. 2016 Jan 15;340(2):220-6. doi: 10.1016/j.yexcr.2015.12.017. Epub 2015 Dec 31. PMID: 26748184 6:The HSP90 inhibitor, NVP-AUY922, sensitizes KRAS-mutant non-small cell lung cancer with intrinsic resistance to MEK inhibitor, trametinib. Park KS, Oh B, Lee MH, Nam KY, Jin HR, Yang H, Choi J, Kim SW, Lee DH.Cancer Lett. 2016 Mar 1;372(1):75-81. doi: 10.1016/j.canlet.2015.12.015. Epub 2015 Dec 23. PMID: 26723875 7:Bioluminescence Imaging to Monitor the Effects of the Hsp90 Inhibitor NVP-AUY922 on NF-κB Pathway in Endometrial Cancer. Yeramian A, García V, Bergadà L, Domingo M, Santacana M, Valls J, Martinez-Alonso M, Carceller JA, Cussac AL, Dolcet X, Matias-Guiu X.Mol Imaging Biol. 2016 Aug;18(4):545-56. doi: 10.1007/s11307-015-0907-8. PMID: 26604096 8:The potent activation of Ca(2+)-activated K(+) current by NVP-AUY922 in the human pancreatic duct cell line (PANC-1) possibly independent of heat shock protein 90 inhibition. Chiang NJ, Wu SN, Chen LT.J Pharmacol Sci. 2015 Apr;127(4):404-13. doi: 10.1016/j.jphs.2015.02.009. Epub 2015 Feb 20. PMID: 25953267 Free Article9:Phase 1/1B trial of the heat shock protein 90 inhibitor NVP-AUY922 as monotherapy or in combination with bortezomib in patients with relapsed or refractory multiple myeloma. Seggewiss-Bernhardt R, Bargou RC, Goh YT, Stewart AK, Spencer A, Alegre A, Bladé J, Ottmann OG, Fernandez-Ibarra C, Lu H, Pain S, Akimov M, Iyer SP.Cancer. 2015 Jul 1;121(13):2185-92. doi: 10.1002/cncr.29339. Epub 2015 Mar 24. PMID: 25809731 Free Article10:Hsp90 inhibitor NVP-AUY922 enhances the radiation sensitivity of lung cancer cell lines with acquired resistance to EGFR-tyrosine kinase inhibitors. Hashida S, Yamamoto H, Shien K, Ohtsuka T, Suzawa K, Maki Y, Furukawa M, Soh J, Asano H, Tsukuda K, Miyoshi S, Kanazawa S, Toyooka S.Oncol Rep. 2015 Mar;33(3):1499-504. doi: 10.3892/or.2015.3735. Epub 2015 Jan 20. PMID: 25607753