For research use only. Not for therapeutic Use.
Triciribine（Cat No.:I003315）is a synthetic purine nucleoside analog that inhibits the Akt signaling pathway, which plays a critical role in cell survival, proliferation, and metabolism. By blocking Akt activation, triciribine induces apoptosis in cancer cells, making it a potential therapeutic agent for various cancers, including breast, lung, and prostate cancers. It has been studied in clinical trials for its ability to enhance the effects of other cancer therapies, particularly in overcoming resistance to chemotherapy and targeted treatments. Although its clinical use has been limited by toxicity, triciribine remains a subject of ongoing cancer research.
| Catalog Number | I003315 |
| CAS Number | 35943-35-2 |
| Synonyms | (2R,3R,4S,5R)-2-(3-amino-5-methyl-1,4,5,6,8-pentaazaacenaphthylen-1(5H)-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol |
| Molecular Formula | C₁₃H₁₆N₆O₄ |
| Purity | ≥95% |
| Target | PI3K/Akt/mTOR |
| Solubility | DMSO: ≥ 44 mg/mL |
| Storage | 3 years -20℃ powder |
| IC50 | 130 nM (Akt); 20 nM (HIV1) |
| IUPAC Name | (2R,3R,4S,5R)-2-(5-amino-7-methyl-2,6,7,9,11-pentazatricyclo[6.3.1.04,12]dodeca-1(12),3,5,8,10-pentaen-2-yl)-5-(hydroxymethyl)oxolane-3,4-diol |
| InChI | InChI=1S/C13H16N6O4/c1-18-11-7-5(10(14)17-18)2-19(12(7)16-4-15-11)13-9(22)8(21)6(3-20)23-13/h2,4,6,8-9,13,20-22H,3H2,1H3,(H2,14,17)/t6-,8-,9-,13-/m1/s1 |
| InChIKey | HOGVTUZUJGHKPL-HTVVRFAVSA-N |
| SMILES | CN1C2=NC=NC3=C2C(=CN3[C@H]4[C@@H]([C@@H]([C@H](O4)CO)O)O)C(=N1)N |
| Reference | </br>1:An Expedient Total Synthesis of Triciribine. Hu C, Ruan Z, Ding H, Zhou Y, Xiao Q.Molecules. 2017 Apr 17;22(4). pii: E643. doi: 10.3390/molecules22040643. PMID: 28420174 Free Article</br>2:Triciribine Phosphate Monohydrate, an AKT Inhibitor, Enhances Gemcitabine Activity in Pancreatic Cancer Cells. Kim R, Yamauchi T, Husain K, Sebti S, Malafa M.Anticancer Res. 2015 Sep;35(9):4599-604. PMID: 26254348 </br>3:The Akt inhibitor, triciribine, ameliorates chronic hypoxia-induced vascular pruning and TGFβ-induced pulmonary fibrosis. Abdalla M, Sabbineni H, Prakash R, Ergul A, Fagan SC, Somanath PR.Br J Pharmacol. 2015 Aug;172(16):4173-88. doi: 10.1111/bph.13203. Epub 2015 Jul 6. PMID: 26033700 Free PMC Article</br>4:Addition of the Akt inhibitor triciribine overcomes antibody resistance in cells from ErbB2/Neu-positive/PTEN-deficient mammary tumors. Wang Q, Ding H, Liu B, Li SH, Li P, Ge H, Zhang K.Int J Oncol. 2014 Apr;44(4):1277-83. doi: 10.3892/ijo.2014.2271. Epub 2014 Jan 21. PMID: 24452693 </br>5:Phase I clinical, pharmacokinetic, and pharmacodynamic study of the Akt-inhibitor triciribine phosphate monohydrate in patients with advanced hematologic malignancies. Sampath D, Malik A, Plunkett W, Nowak B, Williams B, Burton M, Verstovsek S, Faderl S, Garcia-Manero G, List AF, Sebti S, Kantarjian HM, Ravandi F, Lancet JE.Leuk Res. 2013 Nov;37(11):1461-7. doi: 10.1016/j.leukres.2013.07.034. Epub 2013 Aug 6. PMID: 23993427 Free PMC Article</br>6:AKT inhibition by triciribine alone or as combination therapy for growth control of gastroenteropancreatic neuroendocrine tumors. Gloesenkamp CR, Nitzsche B, Ocker M, Di Fazio P, Quint K, Hoffmann B, Scherübl H, Höpfner M.Int J Oncol. 2012 Mar;40(3):876-88. doi: 10.3892/ijo.2011.1256. Epub 2011 Nov 7. PMID: 22075556 </br>7:Preclinical testing of the Akt inhibitor triciribine in T-cell acute lymphoblastic leukemia. Evangelisti C, Ricci F, Tazzari P, Chiarini F, Battistelli M, Falcieri E, Ognibene A, Pagliaro P, Cocco L, McCubrey JA, Martelli AM.J Cell Physiol. 2011 Mar;226(3):822-31. doi: 10.1002/jcp.22407. PMID: 20857426 </br>8:Phase I pharmacokinetic and pharmacodynamic study of triciribine phosphate monohydrate, a small-molecule inhibitor of AKT phosphorylation, in adult subjects with solid tumors containing activated AKT. Garrett CR, Coppola D, Wenham RM, Cubitt CL, Neuger AM, Frost TJ, Lush RM, Sullivan DM, Cheng JQ, Sebti SM.Invest New Drugs. 2011 Dec;29(6):1381-9. doi: 10.1007/s10637-010-9479-2. Epub 2010 Jul 20. PMID: 20644979 Free PMC Article</br>9:Inhibition of human immunodeficiency virus type 1 by triciribine involves the accessory protein nef. Ptak RG, Gentry BG, Hartman TL, Watson KM, Osterling MC, Buckheit RW Jr, Townsend LB, Drach JC.Antimicrob Agents Chemother. 2010 Apr;54(4):1512-9. doi: 10.1128/AAC.01443-09. Epub 2010 Jan 19. PMID: 20086149 Free PMC Article</br>10:The Akt inhibitor triciribine sensitizes prostate carcinoma cells to TRAIL-induced apoptosis. Dieterle A, Orth R, Daubrawa M, Grotemeier A, Alers S, Ullrich S, Lammers R, Wesselborg S, Stork B.Int J Cancer. 2009 Aug 15;125(4):932-41. doi: 10.1002/ijc.24374. PMID: 19422047 Free Article |
