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Triciribine

Cat. No. M1884
Triciribine Structure
Synonym:

API-2, NSC 154020, TCN

Size Price Availability Quantity
5mg USD 90 In stock
10mg USD 140 In stock
50mg USD 450 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Triciribine, also known as API-2, NSC 154020, is a cell-permeable tricyclic nucleoside that inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3. Akt-1, -2, and -3 are serine/threonine protein kinases in the phosphatidylinositol 3 (PI3)-kinase signalling pathway that play a critical role in the regulation of cell proliferation and survival. Triciribine induced autophagy, which could be interpreted as a defensive mechanism, because an autophagy inhibitor (chloroquine) increased triciribine-induced apoptosis. In vitro, Triciribine (API-2) significantly inhibits Akt-overexpressing human cancer cell lines growth with 50% inhibition at ~5-10 µM. It also inhibits DNA synthesis and displays antiviral activity against HIV-1 and -2. Combinations of triciribine with classic inhibitors targeting other molecules of the PI3K-AKT-pathway led to synergistic anti-proliferative effects.

Protocol
Cell Experiment
Cell lines LNCaP, PC-3, OVCAR3, OVCA8, PANC1, MDA-MB-468, and WM35 cells line
Preparation method Screening for Inhibition of Akt-Transformed Cell Growth.
AKT2 transformed NIH3T3 cells or LXSN vector-transfected NIH3T3 control cells (4) were plated into 96-well tissue culture plate. After treatment with 5 μM NCI Diversity Set compound, cell growth was detected with CellTier 96 One Solution Cell Proliferation kit (Promega). Compounds that inhibit growth in AKT2-transformed but not LXSN-transfected NIH3T3 cells were considered as candidates of Akt inhibitor and subjected to additional analysis.
Concentrations 0~20 μM
Incubation time 24 and 48 h
Animal Experiment
Animal models Nude Mouse Tumor Xenograft Model
Formulation 20% DMSO
Dosages 1 mg/kg/day
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 320.3
Formula C13H16N6O4
CAS Number 35943-35-2
Purity >99%
Solubility DMSO
Storage at -20°C
References

AKT inhibition by triciribine alone or as combination therapy for growth control of gastroenteropancreatic neuroendocrine tumors.
Gloesenkamp CR, et al. Int J Oncol. 2012 Mar;40(3):876-88. PMID: 22075556.

Preclinical testing of the Akt inhibitor triciribine in T-cell acute lymphoblastic leukemia.
Evangelisti C, et al. J Cell Physiol. 2011 Mar;226(3):822-31. PMID: 20857426.

Akt/protein kinase B signaling inhibitor-2, a selective small molecule inhibitor of Akt signaling with antitumor activity in cancer cells overexpressing Akt.
Yang L, et al. Cancer Res. 2004 Jul 1;64(13):4394-9. PMID: 15231645.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Triciribine, API-2, NSC 154020, TCN supplier, Akt, inhibitors

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