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    Triciribine
    Triciribine

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0162
    CAS #: 35943-35-2Purity ≥98%

    Description: Triciribine (also known as API-2) is a DNA synthesis inhibitor which also inhibits the phosphorylation level and kinase activity of Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; it does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Triciribine, also known as VQD-002, is a potent AKT inhibitor and a cell-permeable tricyclic nucleoside molecule with potential antineoplastic activity. Triciribine inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3, which may result in the inhibition of Akt-expressing tumor cell proliferation.

    References:  J Cell Mol Med. 2005 Jan-Mar;9(1):59-71; Cancer Res. 2004 Jul 1;64(13):4394-9.

    Related CAS #: 61966-08-3 (Triciribine phosphate)

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    Molecular Weight (MW)

    320.3

    Formula

    C13H16N6O4

    CAS No.

    35943-35-2

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO:64 mg/mL (199.8 mM)

    Water: <1 mg/mL

    Ethanol: 5 mg/mL (14.8 mM)

    Solubility (In vivo)

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

    Chemical Name/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; API-2; API 2; API2; VQD-002; VQD 002; VQD002; NSC-154020; NSC 154020; NSC154020; TCN


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    In Vitro

    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 Assay: 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.

    Triciribine exhibits maximum growth inhibition around 1-10 μM and inhibits phosphorylation of Akt, as well as downstream p70S6K, to basal levels at 100μM (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. Triciribine inihibits HIV-1with an IC50 of 20 nM. Greater than 90% inhibition is achieved at 0.1μM and complete inhibition of syncytia formation is achieved at 5μM. 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. 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. 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.

    In Vivo

    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.

    Animal model

    OVCAR3, OVCAR8, PANC1, OVCAR5 and COLO357 tumor cells are injected s.c. into 80week-old female nude mice.

    Formulation & Dosage

    Dissolved in  20% DMSO; 1 mg/kg; i.p. injection

    References

    [1] Yang L, et al, Cancer Res, 2004, 64(13), 4394-4399.; [2] Neuro Oncol. 2011 Jun;13(6):610-21.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Triciribine

    Identification of API-2 (TCN, triciribine) as a candidate of Akt inhibitor from the NCI Diversity Set. Cancer Res, 2004, 64(13), 4394-4399.



    Triciribine

    API-2 does not inhibit PI3k, PDK1, and the closely related members of AGC kinase family.

    Triciribine

    API-2 inhibits downstream targets of Akt and exhibits antitumor activity in cancer cell lines with elevated Akt in mouse xenograft.


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