Triciribine (API-2)

Catalog No.S1117 Batch:S111703

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Technical Data

Formula

C13H16N6O4
Molecular Weight 320.3 CAS No. 35943-35-2
Solubility (25°C)* In vitro DMSO 64 mg/mL (199.81 mM)
Ethanol 16 mg/mL (49.95 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
2% DMSO 40% PEG 300 5%Tween80 53%ddH2O
1.5mg/ml Taking the 1 mL working solution as an example, add 20 μL of 75 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Triciribine (API-2) is a DNA synthesis inhibitor, also inhibits Akt in PC3 cell line and HIV-1 in CEM-SS, H9, H9IIIB, U1 cells with IC50 of 130 nM and 20 nM, respectively; does not inhibit PI3K/PDK1; 5000-fold less active in cells lacking adenosine kinase. Phase 1/2.
Targets
HIV-1 [2]
(CEM-SS, H9, H9IIIB, U1 cells)		 Akt [1]
(PC3 cells)
20 nM 130 nM
In vitro 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. [1] 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. [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]
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. [4]

Protocol (from reference)

Kinase Assay:[1]
  • 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:[2]
  • Cell lines

    CEM-SS cells

  • Concentrations

    0-500 μM

  • Incubation Time

    48 hours

  • Method

    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.
Animal Study:[4]
  • Animal Models

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

  • Dosages

    1 mg/kg/day

  • Administration

    Triciribine is administrated through i.p. injection once a day.

Customer Product Validation

, , Oncol Lett, 2016, 11(3):1889-1894.

Data from [Data independently produced by , , Biochim Biophys Acta Mol Basis Dis, 2017, 1863(9):2307-2318]

Data from [Data independently produced by , , Oncotarget, 2016, 7(30):48346-48359]

Data from [Data independently produced by , , Oxid Med Cell Longev, 2017, 2017:8519169]

Selleck's Triciribine (API-2) has been cited by 96 publications

Lamin A/C phosphorylation at serine 22 is a conserved heat shock response to regulate nuclear adaptation during stress [ J Cell Sci, 2023, 136(4)jcs259788] PubMed: 36695453
Functional restoration of lysosomes and mitochondria through modulation of AKT activity ameliorates senescence [ Exp Gerontol, 2023, 173:112091] PubMed: 36657533
Regulation of miRNA expression by α4β1 integrin-dependent multiple myeloma cell adhesion [ EJHaem, 2023, 4(3):631-638] PubMed: 37601846
Regulation of miRNA expression by α4β1 integrin-dependent multiple myeloma cell adhesion [ EJHaem, 2023, 4(3):631-638] PubMed: 37601846
CREB3L1 promotes tumor growth and metastasis of anaplastic thyroid carcinoma by remodeling the tumor microenvironment [ Mol Cancer, 2022, 21(1):190] PubMed: 36192735
Disruption of the IL-33-ST2-AKT signaling axis impairs neurodevelopment by inhibiting microglial metabolic adaptation and phagocytic function [ Immunity, 2022, 55(1):159-173.e9] PubMed: 34982959
DENR controls JAK2 translation to induce PD-L1 expression for tumor immune evasion [ Nat Commun, 2022, 13(1):2059] PubMed: 35440133
Anionic nanoplastic exposure induces endothelial leakiness [ Nat Commun, 2022, 13(1):4757] PubMed: 35963861
CRISPR/Cas9 Screens Reveal that Hexokinase 2 Enhances Cancer Stemness and Tumorigenicity by Activating the ACSL4-Fatty Acid β-Oxidation Pathway [ Adv Sci (Weinh), 2022, 9(21):e2105126] PubMed: 35603967
Isoginkgetin, a Potential CDK6 Inhibitor, Suppresses SLC2A1/GLUT1 Enhancer Activity to Induce AMPK-ULK1-Mediated Cytotoxic Autophagy in Hepatocellular Carcinoma [ Autophagy, 2022, 10.1080/15548627.2022.2119353] PubMed: 36048765

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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