Triciribine (API2; NSC 154020; VQD002)

Alias: VQD002; VQD-002; VQD 002; NSC 154020; NSC154020; NSC-154020; Triciribine
Cat No.:V0162 Purity: ≥98%
Triciribine (also known as API-2; NSC-154020; VQD-002), a cell-permeable tricyclic nucleoside molecule, is a potent DNA synthesis inhibitor with potential anticancer activity.
Triciribine (API2; NSC 154020; VQD002) Chemical Structure CAS No.: 35943-35-2
Product category: Akt
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Triciribine (API2; NSC 154020; VQD002):

  • Triciribine phosphate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Triciribine (also known as API-2; NSC-154020; VQD-002), a cell-permeable tricyclic nucleoside molecule, is a potent DNA synthesis inhibitor with potential anticancer activity. Additionally, with an IC50 of 130 nM and 20 nM, respectively, it inhibits Akt (in the PC3 cell line) and HIV-1 (in the CEM-SS, H9, H9IIIB, and U1 cells). Triciribine prevents the phosphorylation, activation, and signaling of Akt-1, -2, and -3, which may prevent the proliferation of tumor cells that express Akt.

Biological Activity I Assay Protocols (From Reference)
Targets
HIV-1 (IC50 = 0.02-0.46 μM); HIV-2 (IC50 = 0.02-0.46 μM); Akt (IC50 = 130 nM); DNA synthesis
ln 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 has the potential to grade-dependently suppress the growth of Nf1 and Trp53 mutant astrocytoma cells. While 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), the WHO II K1861-10 line is only partially inhibited (69% maximum inhibition) by Triciribine. Triciribine is significantly less effective at inhibiting primary astrocytes (GI5013.6 mM), which indicates that this inhibitor might have a preference for tumor cells.[1] Triciribine inihibits HIV-1with an IC50 of 20 nM. At 0.1μM , greater than 90% inhibition is attained, and at 5 μM, total inhibition of syncytia formation is attained. Triciribine has a 46 μM associated cell toxicity in the same cell line, resulting in a selectivity index of 2250. Using HIV-1 acutely infected CEM-SS, H9, and persistently infected H9III B and U1 cells, triciribine significantly reduces the production of p24 core antigen, reverse transcriptase, and infectious virus. [2] Triciribine inhibits Akt phosphorylation at Thr308 and Ser473 and Akt activity in the human prostate cancer cell line PC-3. Triciribine renders PC-3 cells resistant to DNA-damaging chemotherapeutics while making them more susceptible to TRAIL- and anti-CD95-induced apoptosis. [3] Triciribine has a high affinity for Akt but not for phosphatidylinositol 3-kinase, 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]
ln 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. OVCAR5 and COLO357 cell growth, however, is not significantly impacted by triciribine. [4]
Enzyme Assay
Cells are expanded to 80%–90% confluency and stimulated for 5–10 minutes with 1–10 ng/mL of platelet derived growth factor (PDGF)–AA or epidermal growth factor with or without 10–20 mM of U0126 or LY-294002 in order to promote cell growth. Protein lysates (5–20 g) are subjected to 12%–15% SDS PAGE separation before being subjected to a Western blot analysis 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. Triciribine serial fivefold dilutions are prepared in growth medium and added to the wells. Cells are pulse-labeled with [3H]dThd (1 Ci per well, specific activity 20 Ci/mmol) for 6 hours after 48 hours of incubation at 37 °C, and then harvested to determine total DNA synthesis.
Animal Protocol
OVCAR3, OVCAR8, PANC1, OVCAR5 and COLO357 tumor cells are injected s.c. into 80week-old female nude mice.
1 mg/kg/day
Triciribine is administrated through i.p. injection once a day.
References

[1]. Neuro Oncol . 2011 Jun;13(6):610-21.

[2]. AIDS Res Hum Retroviruses . 1993 Apr;9(4):307-14.

[3]. Int J Cancer . 2009 Aug 15;125(4):932-41.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C13H16N6O4
Molecular Weight
320.30394
Exact Mass
320.1233
Elemental Analysis
C, 48.75; H, 5.03; N, 26.24; O, 19.98
CAS #
35943-35-2
Appearance
Tan solid powder
SMILES
CN1C2=NC=NC3=C2C(=CN3[C@H]4[C@@H]([C@@H]([C@H](O4)CO)O)O)C(=N1)N
InChi Key
HOGVTUZUJGHKPL-HTVVRFAVSA-N
InChi Code
InChI=1S/C13H16N6O4/c1-18-11-7-5(10(14)17-18)2-19(12(7)16-4-15-11)13-9(22)8(21)6(3-20)23-13/h2,4,6,8-9,13,20-22H,3H2,1H3,(H2,14,17)/t6-,8-,9-,13-/m1/s1
Chemical Name
(2R,3R,4S,5R)-2-(5-amino-7-methyl-2,6,7,9,11-pentazatricyclo[6.3.1.04,12]dodeca-1(12),3,5,8,10-pentaen-2-yl)-5-(hydroxymethyl)oxolane-3,4-diol
Synonyms
VQD002; VQD-002; VQD 002; NSC 154020; NSC154020; NSC-154020; Triciribine
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
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 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.1221 mL 15.6104 mL 31.2207 mL
5 mM 0.6244 mL 3.1221 mL 6.2441 mL
10 mM 0.3122 mL 1.5610 mL 3.1221 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Status Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05691556 Recruiting Procedure: HABIT ILE
rehabilitation course
Procedure: botulinum
toxin injections
Cerebral Palsy Infantile University Hospital, Brest July 16, 2020
Biological Data
  • 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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