NVP-HSP990

• CAT Number: I005544
• CAS Number: 934343-74-5
• Molecular Formula: C20H18FN5O2
• Molecular Weight: 379.40
• Purity: ≥95%
• Synonyms: (7R)-2-amino-7-[4-fluoro-2-(6-methoxypyridin-2-yl)phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one
• Target: HSP
• Solubility: DMSO: ≥ 33 mg/mL
• Storage: Store at -20°C
• IC50: 13 nM(Hsp90α)
• InChI: InChI=1S/C20H18FN5O2/c1-10-18-16(26-20(22)23-10)9-15(25-19(18)27)12-7-6-11(21)8-13(12)14-4-3-5-17(24-14)28-2/h3-8,15H,9H2,1-2H3,(H,25,27)(H2,22,23,26)/t15-/m1/s1
• InChIKey: WSMQUUGTQYPVPD-OAHLLOKOSA-N
• SMILES: CC1=C2C(=NC(=N1)N)C[C@@H](NC2=O)C3=C(C=C(C=C3)F)C4=NC(=CC=C4)OC

NVP-HSP990（Cat No.:I005544）is a selective inhibitor of heat shock protein 90 (HSP90), a molecular chaperone that assists in the proper folding and stabilization of client proteins, many of which are involved in cancer progression. By inhibiting HSP90, NVP-HSP990 disrupts the function of these client proteins, leading to cancer cell apoptosis and impaired tumor growth. It has shown potential in preclinical studies against various malignancies, including solid tumors and hematological cancers. Its selectivity and ability to target multiple signaling pathways make it a promising candidate for cancer therapy.

Reference

1:Retraction: Novel HSP90 inhibitor NVP-HSP990 targets cell-cycle regulators to ablate Olig 2-positive glioma tumor-initiating cells. Koul D, Yao J, Wan S, Yuan Y, Sulman E, Lang F, Yung WK, Colman H.Cancer Res. 2014 Nov 15;74(22):6731-2. doi: 10.1158/0008-5472.CAN-14-2966. No abstract available. PMID: 25398854 Free PMC Article2:Design, structure-activity relationship, and in vivo characterization of the development candidate NVP-HSP990. McBride CM, Levine B, Xia Y, Bellamacina C, Machajewski T, Gao Z, Renhowe P, Antonios-McCrea W, Barsanti P, Brinner K, Costales A, Doughan B, Lin X, Louie A, McKenna M, Mendenhall K, Poon D, Rico A, Wang M, Williams TE, Abrams T, Fong S, Hendrickson T, Lei D, Lin J, Menezes D, Pryer N, Taverna P, Xu Y, Zhou Y, Shafer CM.J Med Chem. 2014 Nov 13;57(21):9124-9. doi: 10.1021/jm501107q. Epub 2014 Nov 4. PMID: 25368984 3:Novel HSP90 inhibitor NVP-HSP990 targets cell-cycle regulators to ablate Olig2-positive glioma tumor-initiating cells. Fu J, Koul D, Yao J, Wang S, Yuan Y, Colman H, Sulman EP, Lang FF, Yung WK.Cancer Res. 2013 May 15;73(10):3062-74. doi: 10.1158/0008-5472.CAN-12-2033. Epub 2013 Mar 14. Retraction in: Koul D, Yao J, Wan S, Yuan Y, Sulman E, Lang F, Yung WK, Colman H. Cancer Res. 2014 Nov 15;74(22):6731-2. PMID: 23492364 Free PMC Article4:Increased radiosensitivity and radiothermosensitivity of human pancreatic MIA PaCa-2 and U251 glioblastoma cell lines treated with the novel Hsp90 inhibitor NVP-HSP990. Milanović D, Firat E, Grosu AL, Niedermann G.Radiat Oncol. 2013 Feb 28;8:42. doi: 10.1186/1748-717X-8-42. PMID: 23448094 Free PMC Article5:The novel, orally bioavailable HSP90 inhibitor NVP-HSP990 induces cell cycle arrest and apoptosis in multiple myeloma cells and acts synergistically with melphalan by increased cleavage of caspases. Lamottke B, Kaiser M, Mieth M, Heider U, Gao Z, Nikolova Z, Jensen MR, Sterz J, von Metzler I, Sezer O.Eur J Haematol. 2012 May;88(5):406-15. doi: 10.1111/j.1600-0609.2012.01764.x. Epub 2012 Mar 21. PMID: 22309072 6:Preclinical activity of the novel orally bioavailable HSP90 inhibitor NVP-HSP990 against multiple myeloma cells. Stühmer T, Iskandarov K, Gao Z, Bumm T, Grella E, Jensen MR, Einsele H, Chatterjee M, Bargou RC.Anticancer Res. 2012 Feb;32(2):453-62. PMID: 22287732 7:The novel oral Hsp90 inhibitor NVP-HSP990 exhibits potent and broad-spectrum antitumor activities in vitro and in vivo. Menezes DL, Taverna P, Jensen MR, Abrams T, Stuart D, Yu GK, Duhl D, Machajewski T, Sellers WR, Pryer NK, Gao Z.Mol Cancer Ther. 2012 Mar;11(3):730-9. doi: 10.1158/1535-7163.MCT-11-0667. Epub 2012 Jan 12. PMID: 22246440 Free Article