产品编号 T6065   CAS 35943-35-2
别名: NSC 154020, TCN, API-2, VD-0002, Tricyclic nucleoside, VD-0002, Tricyclic nucleoside, TCN, NSC 154020 API-2

Triciribine is a DNA synthesis inhibitor, and it also inhibits Akt and HIV-1/2.

Triciribine , CAS 35943-35-2
规格 库存 价格/RMB 数量
2 mg 上海现货 420.00
5 mg 上海现货 810.00
10 mg 上海现货 1120.00
25 mg 上海现货 2260.00
50 mg 上海现货 3880.00
100 mg 上海现货 6984.00
1 mL * 10 mM (in DMSO) 上海现货 810.00
纯度 99.87%
纯度 100.00%
存储 & 溶解度
Preparing Solutions
产品描述 Triciribine is a DNA synthesis inhibitor, and it also inhibits Akt and HIV-1/2.
靶点活性 Akt : ic50 130nM ,   HIV-1 : ic50 20nM
体外活性 Triciribine exhibits maximum growth inhibition around 1-10 μM and inhibits phosphorylation of Akt, as well as downstream p70S6K, to basal levels at 100 μM (IC50 = 130 nM). Triciribine shows particular promise for inhibiting growth in Nf1 and Trp53 mutant astrocytoma cells in a grade-dependent manner. The WHO II K1861-10 line is inhibited, incompletely (69% maximum inhibition), with a GI50 value of 1.7 μM for Triciribine, whereas higher-grade tumor lines (KR158, KR130, and SF295) are inhibited to a greater extent (>80% maximum inhibition) at lower GI50 values (0.4–1.1 mM). Importantly, Triciribine is much less effective at inhibiting primary astrocytes (GI5013.6 mM), suggesting that this inhibitor may show specificity for tumor cells. [1] Triciribine inihibits HIV-1with an IC50 of 20 nM. Greater than 90% inhibition is achieved at 0.1 μM and complete inhibition of syncytia formation is achieved at 5 μM. Associated cell toxicity in the same cell line for Triciribine is 46 μM, resulting in selectivity indices of 2250. Triciribine markedly inhibits HIV-1-induced p24 core antigen production, reverse transcriptase, and infectious virus production in a dose-dependent manner using HIV-1 acutedly infected CEM-SS, H9, and persistently infected H9III B and U1 cells. [2] Triciribine inhibits Akt phosphorylation at Thr308 and Ser473 and Akt activity in the human prostate cancer cell line PC-3. Triciribine sensitizes PC-3 cells to TRAIL- and anti-CD95-induced apoptosis, whereas the cells remain resistant to DNA damaging chemotherapeutics. [3] Triciribine is highly selective for Akt and does not inhibit the activation of phosphatidylinositol 3-kinase, phosphoinositide-dependent kinase-1, protein kinase C, serum and glucocorticoid-inducible kinase, protein kinase A, signal transducer and activators of transcription 3, extracellular signal-regulated kinase-1/2, or c-Jun NH2-terminal kinase. [4]
体内活性 1 mg/kg/day i.p. treated Triciribine inhibits OVCAR3, OVCAR8 and PANC1 tumor growth, which overexpressing Akt, by 90%, 88% and 80% in nude mice, respectively. However, Triciribine has little effect on the growth of OVCAR5 and COLO357 cells. [4]
Kinase Assay Akt Phosphorylation Changes Assay: Cells are grown to 80%–90% confluency and stimulated for 5–10 minutes with 1–10 ng/mL of epidermal growth factor or platelet derived growth factor (PDGF)–AA with or without 10–20 mM of U0126 or LY-294002. Protein lysates (5–20 μg) are separated by 12%–15% SDS PAGE and analyzed by Western blot for Akt, phosphorylated Akt (phospho-Ser 473), MAPK, and phosphorylated MAPK (p44/42 phospho-Thr202/Tyr204) antibodies (1:1000).
Cell Research
Triciribine is evaluated for cytotoxicity by seeding CEM-SS cells at a density of 1 × 104 cells/well in growth medium, using a 96-well flat-bottom plate. Serial fivefold dilutions of Triciribine are prepared in growth medium and added to the wells as a second overlay. After a 48-hours incubation at 37 °C, the cells are pulse labeled with [3H]dThd (1 μCi per well, specific activity 20 Ci/mmol) for 6 hours and the cells are harvested to measure total DNA synthesis.(Only for Reference)
Cell lines: CEM-SS cells
Animal Research
Animal Model: OVCAR3, OVCAR8, PANC1, OVCAR5 and COLO357 tumor cells are injected s.c. into 80week-old fenude mice.
别名 NSC 154020 , TCN , API-2 , VD-0002 , Tricyclic nucleoside , VD-0002 , Tricyclic nucleoside , TCN , NSC 154020 API-2
纯度 100.00%
分子量 320.3
分子式 C13H16N6O4
CAS No. 35943-35-2


0-4℃ for short term (days to weeks), or -20℃ for long term (months).


1eq. HCl: 32 mg/mL (100 mM)

DMSO: 32 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

1% DMSO/30% polyethylene glycol/1% Tween 80: 30 mg/mL


1. Gursel DB, et al, Nero Oncol, 2011, 13(6), 610-621. 2. Kucera LS, et al, AIDS Res Hum Retroviruses, 1993, 9(4), 307-314. 3. Dieterle A, et al, Int J Cancer , 2009, 125(4), 932-941. 4. Yang L, et al, Cancer Res, 2004, 64(13), 4394-4399. 5. Abdalla M, et al. The Akt inhibitor, triciribine, ameliorates chronic hypoxia-induced vascular pruning and TGFβ-induced pulmonary fibrosis. Br J Pharmacol. 2015 Aug;172(16):4173-88.

Related Compound Libraries

This product is contained In the following compound libraries:
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Karanjin RN-18 A-674563 2HCl(552325-73-2(fb-2hcl)) Triciribine AT7867 Liquidambaric lactone Ilexgenin A Cytochalasin D


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