Triciribine

Catalog No.S1117

Triciribine 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.

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Triciribine Chemical Structure

Triciribine Chemical Structure
Molecular Weight: 320.3

Validation & Quality Control

Quality Control & MSDS

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Triciribine is available in the following compound libraries:

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Product Description

Biological Activity

Description Triciribine 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)
IC50 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]
Features

Protocol(Only for 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).
Assays for reverse transcriptase activity and p24 core antigen production Virus particles are precipitated from cell-free supernatant as follows: 0.3 mL of 4 M NaCl and 3.6 ml of 30% (wt/vol) polyethylene glycol are added to 7.5 mL of particle-containing medium and the suspension is placed on ice for 2 hours. The suspension is

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.
Formulation Triciribine is dissolved in 20% DMSO.
Dosages 1 mg/kg/day
Administration Triciribine is administrated through i.p. injection once a day.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Gursel DB, et al, Nero Oncol, 2011, 13(6), 610-621.

[2] Kucera LS, et al, AIDS Res Hum Retroviruses, 1993, 9(4), 307-314.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01690468 Active, not recruiting Ovarian Cancer Prescient Therapeutics, Ltd.|United States Department of  ...more Prescient Therapeutics, Ltd.|United States Department of Defense|Virax Pty. Ltd, September 2014 Phase 1|Phase 2
NCT01697293 Recruiting Breast Adenocarcinoma|Estrogen Receptor Positive|HER2/Neu Negative|Recurrent Breast Carcinoma|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|Stag  ...more Breast Adenocarcinoma|Estrogen Receptor Positive|HER2/Neu Negative|Recurrent Breast Carcinoma|Stage IIB Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer Albert Einstein College of Medicine of Yeshiva University  ...more Albert Einstein College of Medicine of Yeshiva University|National Cancer Institute (NCI) January 2012 Phase 1|Phase 2
NCT00642031 Completed Hematologic Malignancies|Leukemia M.D. Anderson Cancer Center|VioQuest Pharmaceuticals August 2006 Phase 1
NCT00363454 Completed Cancer Prescient Therapeutics, Ltd.|VioQuest Pharmaceuticals April 2006 Phase 1

Chemical Information

Download Triciribine SDF
Molecular Weight (MW) 320.3
Formula

C13H16N6O4

CAS No. 35943-35-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms NSC 154020, VD-0002, vqd-002
Solubility (25°C) * In vitro DMSO 64 mg/mL (199.81 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL
* <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.
Chemical Name 6-Amino-4-methyl-8-(β-D-ribofuranosyl)-4H,8H-pyrrolo[4,3,2-de]pyrimido[4,5-c]pyridazine

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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