- 英文名称
- triciribine
- 分子式
- C13H16N6O4
- 分子量
- 320.3
- 中文别名
- (2R,3R,4S,5R)-2-(3-氨基-5-甲基-1,4,5,6,8-五氮杂苊烯-1(5H)-基)-5-(羟甲基)四氢呋喃-3,4-二醇; 曲西瑞宾; 1,5-二氢-5-甲基-1-BETA-D-呋喃核糖基-1,4,5,6,8-五氮杂苊-3-胺; (2R,3R,4S,5R)-2-(3-Amino-5-methyl-1,4,5,6,8-pentaazaacenaphthylen-1(5H)-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol; API-2; 5-Methyl-1-(β-D-ribofuranosyl)-1,5-dihydro-1,4,5,6,8-pentaazaacenaphthylen-3-amine; 1,5-Dihydro-5-methyl-1-β-D-ribofuranosyl-1,4,5,6,8-pentaazaacenaphthylen-3-amine; 1,5-Dihydro-5-methyl-1-b-D-ribofuranosyl-1,4,5,6,8-pentaazaacennaphthylen-3-amine; 5-Methyl-1-b-D-ribofuranosyl-1,5-dihydro-1,4,5,6,8-pentaazaacenaphthylen-3-amine; 6-AMINO-4-METHYL-8-(BETA-D-RIBOFURANOSYL)-4H,8H-PYRROLO[4,3,2-DE]PYRIMIDO[4,5-C]PYRIDAZINE; AKT/PKB SIGNALING INHIBITOR-2; AKT INHIBITOR V; 1,4,5,6,8-pentaazaacenaphthylen-3-amine,1,5-dihydro-5-methyl-1-beta-d-ribofura; API-2 (Tricirbine)
- 用途
- 曲西瑞宾是一种小分子DNA合成抑制剂，能抑制Akt和HIV-1的IC50分别为130nM和20nM；对PI3K/PDK1无抑制作用；作用于缺乏腺苷激酶的细胞，活性降低5000倍。低浓度时具有抗病毒和抗肿瘤活性，能强效抑制高表达Akt的移植瘤小鼠中的肿瘤生长，降低高度Akt磷酸化的黑素瘤细胞存活，并提高ad-PUMA介导的抑制肿瘤生长作用；与ad-PUMA联合使用时显著抑制体内人黑素瘤生长，已用于黑素瘤患者的II期临床实验。美国研究发现其能够延缓或逆转致死性肺纤维化和肺动脉高压病。
