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Triciribine Sale

(Synonyms: 曲西瑞宾,API-2; NSC 154020; TCN) 目录号 : GC15392

Triciribine是一种腺苷类似物,靶向抑制蛋白激酶B(Akt),IC50值为130nM,具有抗肿瘤活性。

Triciribine Chemical Structure

Cas No.:35943-35-2

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Description

Triciribine is an adenosine analog that targets protein kinase B (Akt) with an IC50 value of 130nM and has antitumor activity[1, 2]. Triciribine is a DNA synthesis inhibitor of HIV-1 with an IC50 value of 20nM[3].

In vitro, treatment of prostate cancer PC-3 cells with Triciribine (10μM) for 24h enhanced apoptosis induced by TNF-related apoptosis-inducing ligand (TRAIL) and anti-CD95[4]. Treatment of bovine cumulus-oocyte complex (COC) with Triciribine (1μM) for 22h resulted in an increase in the rate of blastocyst formation and increased the in vitro yield of bovine embryos[5].

In vivo, treatment of C57BL/6 J mice with Triciribine (1, 2mg/kg/day) by intraperitoneal injection for 2 weeks significantly increased the level of low-density lipoprotein receptor (LDLR) in the liver of mice[6]. Triciribine (1mg/kg/day) was intraperitoneally injected into mice inoculated with GFP+ Huh7 cells for 14 days, which significantly inhibited the growth of tumors in mice and exerted a synergistic effect when combined with rosiglitazone[7].

References:
[1] Barrichon M, Hadi T, Wendremaire M, et al. EXPRESSION OF CONCERN: Dose‐dependent biphasic leptin‐induced proliferation is caused by non‐specific IL‐6/NF‐κB pathway activation in human myometrial cells[J]. British Journal of Pharmacology, 2015, 172(12): 2974-2990.
[2] Garrett C R, Coppola D, Wenham R M, et al. 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[J]. Investigational new drugs, 2011, 29: 1381-1389.
[3] KUCERA L S, IYER N P, PUCKETT S H, et al. Activity of triciribine and triciribine-5′-monophosphate against human immunodeficiency virus types 1 and 2[J]. AIDS research and human retroviruses, 1993, 9(4): 307-314.
[4] Dieterle A, Orth R, Daubrawa M, et al. The Akt inhibitor triciribine sensitizes prostate carcinoma cells to TRAIL‐induced apoptosis[J]. International journal of cancer, 2009, 125(4): 932-941.
[5] Curcio A G, Ribeiro T I S, Gomes H F, et al. Increased in vitro production of bovine embryos resulting from oocyte maturation in the presence of triciribine, a specific inhibitor of AKT[J]. Theriogenology, 2025, 231: 222-227.
[6] Bjune K, Wierød L, Naderi S. Triciribine increases LDLR expression and LDL uptake through stabilization of LDLR mRNA[J]. Scientific Reports, 2018, 8(1): 16174.
[7] Liu L, Yang Z, Xu Y, et al. Inhibition of oxidative stress-elicited AKT activation facilitates PPARγ agonist-mediated inhibition of stem cell character and tumor growth of liver cancer cells[J]. PloS one, 2013, 8(8): e73038.

Triciribine是一种腺苷类似物,靶向抑制蛋白激酶B(Akt),IC50值为130nM,具有抗肿瘤活性[1, 2]。Triciribine是HIV-1的DNA合成抑制剂,IC50值为20nM[3]

在体外,Triciribine(10μM)处理前列腺癌PC-3细胞24h,增强了TNF相关凋亡诱导配体(TRAIL)和抗CD95诱导的细胞凋亡[4]。Triciribine(1μM)处理牛卵丘-卵母细胞复合物(COC)22h,导致囊胚生成速率增加,增加了牛胚胎的体外产量[5]

在体内,Triciribine(1, 2mg/kg/day)通过腹腔注射处理C57BL/6 J小鼠2周,显著增加了小鼠体内肝脏内低密度脂蛋白受体(LDLR)的水平[6]。Triciribine(1mg/kg/day)通过腹腔注射治疗接种GFP+ Huh7细胞的小鼠14天,显著抑制了小鼠体内肿瘤的生长,与罗格列酮联合治疗发挥协同效应[7]

实验参考方法

Cell experiment [1]:

Cell lines

PC-3 cells

Preparation Method

PC-3 cells were treated with TNF-related apoptosis inducing ligand (TRAIL) (0.1, 1, 10, or 40ng/mL) or anti-CD95 (0.1, 1, 10, or 100ng/mL) in the presence or absence of either Triciribine (10μM) or Akti-1/2 (10μM) for 24h. As control PC-3 cells were treated with Triciribine (0.1, 1, 10 or 40μM) or Akti-1/2 (0.1, 1, 10 or 40μM). Apoptosis was assessed by propidium iodide staining of hypodiploid apoptotic nuclei and flow cytometry.

Reaction Conditions

10μM; 24h

Applications

Triciribine amplifies TRAIL-induced and anti-CD95-induced apoptosis in PC-3 cells.

Animal experiment [2]:

Animal models

C57BL/6 J mice

Preparation Method

Mice were separated into three treatment groups each consisting of 4 mice. One group received i.p. Triciribine at 1mg/kg daily. A second group received daily i.p. injections of Triciribine at 2mg/kg. A third group was administered daily i.p. injections of vehicle (0.1% DMSO in PBS). Injection volumes were 100µL per mouse. Two weeks later, mice were sacrificed and livers were processed into a powder by grinding in liquid nitrogen, lysed in RIPA buffer and then analyzed by Western blotting.

Dosage form

1, 2mg/kg/day; 2 weeks; i.p.

Applications

Treatment of mice with either doses of Triciribine for two weeks significantly increased the levels of hepatic Low-density lipoprotein receptor (LDLR).

References:
[1] Dieterle A, Orth R, Daubrawa M, et al. The Akt inhibitor triciribine sensitizes prostate carcinoma cells to TRAIL?induced apoptosis[J]. International journal of cancer, 2009, 125(4): 932-941.
[2]Bjune K, Wierød L, Naderi S. Triciribine increases LDLR expression and LDL uptake through stabilization of LDLR mRNA[J]. Scientific Reports, 2018, 8(1): 16174.

化学性质

Cas No. 35943-35-2 SDF
别名 曲西瑞宾,API-2; NSC 154020; TCN
化学名 (2R,3R,4S,5R)-2-(3-amino-5-methyl-1,4,5,6,8-pentaazaacenaphthylen-1(5H)-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol
Canonical SMILES [H][C@](N1C(N=C([H])N=C2N(C([H])([H])[H])N=C3N([H])[H])=C2C3=C1[H])([C@]4([H])O[H])O[C@@](C([H])([H])O[H])([H])[C@@]4([H])O[H]
分子式 C13H16N6O4 分子量 320.3
溶解度 ≥ 118.4mg/mL in DMSO 储存条件 Store at -20°C
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1 mM 3.1221 mL 15.6104 mL 31.2207 mL
5 mM 0.6244 mL 3.1221 mL 6.2441 mL
10 mM 0.3122 mL 1.561 mL 3.1221 mL
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