Triciribine

CAS No. 35943-35-2

Triciribine( API 2 | NSC 154020 | Tricyclic Nucleoside )

Catalog No. M14234 CAS No. 35943-35-2

Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1 with IC50 of 130 nM and 20 nM, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 47 In Stock
5MG 77 In Stock
10MG 123 In Stock
25MG 224 In Stock
50MG 374 In Stock
100MG 557 In Stock
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Biological Information

  • Product Name
    Triciribine
  • Note
    Research use only, not for human use.
  • Brief Description
    Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1 with IC50 of 130 nM and 20 nM, respectively.
  • Description
    Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1 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.(In Vitro):The nucleoside analog Triciribine (TCN) is a purine analog which is initially shown to inhibit DNA synthesis. Triciribine selectively inhibits the phosphorylation and activation of all three Akt isoforms. At a concentration of 10 μM Triciribine Akt phosphorylation is inhibited at both Thr308 and Ser473. Triciribine effectively inhibits the phosphorylation and consequently the catalytic activity of Akt in PC-3 cells. The Akt inhibitor Triciribine (TCN) does not effectively inhibit the human cell line U87MG but inhibits other astrocytoma cell lines in a grade-dependent manner. The WHO II K1861-10 line is incompletely inhibited (69% maximum inhibition) with a GI50 value of 1.7 μM for Triciribine. 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) in KR158 cells. Triciribine (TCN) is a novel tricyclic compound with known antitumor activity. Using a syncytial plaque assay, Triciribine is active against HIV-1 at 0.01-0.02 μM. Using a microtiter XTT assay, Triciribine is active against a panel of HIV-1 and HIV-2 strains at IC50 values ranging from 0.02 to 0.46 μM.(In Vivo):Triciribine (TCBN) treatment, administered for 7 days after 14 days of hypoxia until 21 days of hypoxia is reached, reversed the vascular thickening as shown by immunohistochemistry and Western analyses. On the other hand, Rapamycin treatment did not prevent hypoxia-induced pulmonary alveolar haemorrhage and congestion. Triciribine partially inhibits progressive pruning of the vasculature.
  • In Vitro
    The nucleoside analog Triciribine (TCN) is a purine analog which is initially shown to inhibit DNA synthesis. Triciribine selectively inhibits the phosphorylation and activation of all three Akt isoforms. At a concentration of 10 μM Triciribine Akt phosphorylation is inhibited at both Thr308 and Ser473. Triciribine effectively inhibits the phosphorylation and consequently the catalytic activity of Akt in PC-3 cells. The Akt inhibitor Triciribine (TCN) does not effectively inhibit the human cell line U87MG but inhibits other astrocytoma cell lines in a grade-dependent manner. The WHO II K1861-10 line is incompletely inhibited (69% maximum inhibition) with a GI50 value of 1.7 μM for Triciribine. 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) in KR158 cells. Triciribine (TCN) is a novel tricyclic compound with known antitumor activity. Using a syncytial plaque assay, Triciribine is active against HIV-1 at 0.01-0.02 μM. Using a microtiter XTT assay, Triciribine is active against a panel of HIV-1 and HIV-2 strains at IC50 values ranging from 0.02 to 0.46 μM.
  • In Vivo
    Triciribine (TCBN) treatment, administered for 7 days after 14 days of hypoxia until 21 days of hypoxia is reached, reversed the vascular thickening as shown by immunohistochemistry and Western analyses. On the other hand, Rapamycin treatment did not prevent hypoxia-induced pulmonary alveolar haemorrhage and congestion. Triciribine partially inhibits progressive pruning of the vasculature.
  • Synonyms
    API 2 | NSC 154020 | Tricyclic Nucleoside
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    Akt
  • Recptor
    Akt| HIV-1
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    35943-35-2
  • Formula Weight
    320.3
  • Molecular Formula
    C13H16N6O4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:64 mg/mL (199.81 mM); Ethanol:<1 mg/mL (<1 mM); Water:<1 mg/mL (<1 mM)
  • SMILES
    O[C@H]1[C@H](N2C=C3C(N)=NN(C)C4=NC=NC2=C34)O[C@H](CO)[C@H]1O
  • Chemical Name
    (2R,3R,4S,5R)-2-(3-amino-5-methyl-1,4,5,6,8-pentaazaacenaphthylen-1(5H)-yl)-5-(hydroxymethyl)tetrahydrofuran-3,4-diol.

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Gursel DB, et al, Nero Oncol, 2011, 13(6), 610-62
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