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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. 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.
| Targets |
HIV-1 (IC50 = 0.02-0.46 μM); HIV-2 (IC50 = 0.02-0.46 μM); Akt (IC50 = 130 nM); DNA synthesis
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|---|---|
| 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]
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| 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]
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| 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).
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| 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.
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| 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 | |
| Additional Infomation |
Triciribine is a nucleoside analogue in which the nucleobase portion is a 1,4,5,6,8-pentaazaacenaphthylene ring system substituted with an amino group at position 3, and a methyl group at position 5 and is bound to the beta-D-ribofuranosyl moiety by an N(1)-glycosidic linkage. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor.
Triciribine has been used in trials studying the treatment of Leukemia, Ovarian Cancer, HER2/Neu Negative, Breast Adenocarcinoma, and Stage IV Breast Cancer, among others. |
| Molecular Formula |
C13H16N6O4
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|---|---|
| Molecular Weight |
320.30394
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| Exact Mass |
320.123
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| Elemental Analysis |
C, 48.75; H, 5.03; N, 26.24; O, 19.98
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| CAS # |
35943-35-2
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| Related CAS # |
Triciribine phosphate;61966-08-3
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| PubChem CID |
65399
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| Appearance |
Light yellow to khaki Tan solid powder
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| Density |
2.0±0.1 g/cm3
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| Boiling Point |
718.5±70.0 °C at 760 mmHg
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| Flash Point |
388.3±35.7 °C
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| Vapour Pressure |
0.0±2.4 mmHg at 25°C
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| Index of Refraction |
1.928
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| LogP |
-2.7
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
507
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| Defined Atom Stereocenter Count |
4
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| SMILES |
OC[C@H]1OC([C@H](O)[C@@H]1O)N2C3=C(C(C(N)=NN4C)=C2)C4=NC=N3
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| InChi Key |
HOGVTUZUJGHKPL-HTVVRFAVSA-N
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| 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
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| 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
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| Synonyms |
VQD002; VQD-002; VQD 002; NSC 154020; NSC154020; NSC-154020; Triciribine
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~64 mg/mL (~199.8 mM)
Water: <1 mg/mL Ethanol: ~5 mg/mL (~14.8 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL |
| 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.
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.
(2) Be sure to add the solvent(s) in order.
| 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 |
Identification of API-2 (TCN, triciribine) as a candidate of Akt inhibitor from the NCI Diversity Set. Cancer Res, 2004, 64(13), 4394-4399. |
API-2 does not inhibit PI3k, PDK1, and the closely related members of AGC kinase family. |
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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