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| Targets |
Triciribine phosphate sodium targets multiple molecular entities: the three AKT isoforms (AKT1/PKBα, AKT2/PKBβ, AKT3/PKBγ), amidophosphoribosyltransferase, and IMP dehydrogenase. AKT is a serine/threonine kinase that is a central node in the PI3K/AKT/mTOR signaling pathway, which regulates cell proliferation, survival, metabolism, and angiogenesis. AKT is frequently hyperactivated in cancer, making it an important therapeutic target. Triciribine phosphate sodium is a non-ATP competitive allosteric inhibitor of AKT, meaning it binds to a site distinct from the ATP-binding pocket. Amidophosphoribosyltransferase is the rate-limiting enzyme in de novo purine biosynthesis, and IMP dehydrogenase is the rate-limiting enzyme in guanosine nucleotide synthesis. By inhibiting these enzymes, the compound depletes nucleotide pools and inhibits cell proliferation. The compound's multi-targeted mechanism contributes to its anticancer activity.
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| ln Vitro |
In vitro, Triciribine phosphate sodium inhibits the activity of all three AKT isoforms through an allosteric mechanism. It inhibits amidophosphoribosyltransferase, affecting the first committed step of de novo purine biosynthesis. It also inhibits IMP dehydrogenase, the first committed step of guanosine nucleotide synthesis. These inhibitory activities result in antiproliferative and pro-apoptotic effects in cancer cells. The compound's ability to inhibit AKT signaling leads to reduced phosphorylation of downstream targets such as GSK3β, FOXO, and mTOR, and to increased apoptosis. The inhibition of purine biosynthesis depletes nucleotide pools, further inhibiting cell proliferation. The compound has been studied in various cancer cell lines, where it demonstrates antiproliferative activity. However, specific quantitative data such as IC50 values for AKT inhibition or cell proliferation inhibition have not been extensively reported in the available literature.
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| ln Vivo |
In vivo activity of Triciribine phosphate sodium has been studied in the context of cancer. As an AKT inhibitor and purine biosynthesis inhibitor, the compound would be expected to inhibit tumor growth in vivo. The compound is a phosphate salt form of triciribine, which has been studied in clinical trials for its anticancer activity. However, specific details regarding animal model studies, dosing regimens, and quantitative outcomes for Triciribine phosphate sodium itself are limited in the available literature. The compound is intended for research use and has been evaluated in preclinical studies for its potential as an anticancer agent. Further in vivo studies would be required to fully characterize its efficacy, safety, and pharmacokinetic properties in various cancer models.
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| Enzyme Assay |
In vitro enzyme assay protocols for Triciribine phosphate sodium would typically involve measuring its inhibition of AKT kinase activity, amidophosphoribosyltransferase activity, and IMP dehydrogenase activity. For AKT inhibition, a standard protocol would involve incubating recombinant AKT isoforms with varying concentrations of Triciribine phosphate sodium (typically 0.1 nM to 10 μM) and a peptide substrate (e.g., Crosstide or GSK3-derived peptide) in kinase assay buffer containing ATP. Phosphorylation of the substrate is detected using methods such as 33P-ATP incorporation, TR-FRET, or luminescent kinase assays. IC50 values are determined from concentration-response curves. For amidophosphoribosyltransferase inhibition, assays measure the conversion of phosphoribosyl pyrophosphate (PRPP) and glutamine to phosphoribosylamine (PRA) and glutamate, with detection by HPLC or colorimetric methods. For IMP dehydrogenase inhibition, assays measure the conversion of IMP to XMP with NAD+ as cofactor, with detection by spectrophotometry.
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| Cell Assay |
In vitro cell-based assay protocols for Triciribine phosphate sodium would typically involve assessing its effects on cell proliferation, AKT signaling, and nucleotide biosynthesis in cultured cancer cells. A standard protocol would involve seeding cancer cells (e.g., breast, ovarian, or pancreatic cancer cells) in multi-well plates and treating them with varying concentrations of Triciribine phosphate sodium (typically 0.1 nM to 10 μM) for 24-72 hours. Cell proliferation is measured using MTT, CCK-8, or BrdU incorporation assays. AKT signaling is assessed by Western blot analysis of phosphorylated AKT (Ser473 and Thr308) and downstream targets such as GSK3β, FOXO, and mTOR. Nucleotide levels can be assessed by HPLC or LC-MS. Apoptosis can be assessed by Annexin V staining or caspase activity assays. Appropriate controls include vehicle-treated cells.
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| Animal Protocol |
In vivo animal experimental protocols for Triciribine phosphate sodium would typically involve administering the compound to tumor-bearing mice in xenograft models. A standard protocol would involve implanting cancer cells (e.g., breast or ovarian cancer cells) subcutaneously in immunodeficient mice, allowing tumors to reach a certain size, and then administering Triciribine phosphate sodium via intraperitoneal or intravenous injection at doses determined from preliminary pharmacokinetic and tolerability studies (e.g., 1-20 mg/kg). Treatment would typically be administered daily or every other day for 2-4 weeks. Endpoints would include tumor volume measurement, tumor weight at necropsy, assessment of AKT phosphorylation and downstream signaling in tumor tissues, assessment of nucleotide levels, and evaluation of apoptosis. Appropriate controls would include vehicle-treated groups. The compound's anticancer activity has been evaluated in preclinical studies, but specific published protocols are limited.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Triciribine phosphate sodium have been characterized to some extent in the context of its development as an anticancer agent. As a phosphate prodrug, the compound is designed to be converted to its active form, triciribine, by cellular phosphatases. The phosphate salt form enhances solubility for parenteral administration. The compound has the molecular formula C13H16N6NaO7P and a molecular weight of 422.27. Specific PK parameters such as half-life, Cmax, AUC, bioavailability, volume of distribution, and clearance have been reported in preclinical studies but are not extensively detailed in the available literature. The compound should be stored under nitrogen, away from moisture, at -20°C. Further pharmacokinetic studies would be required to fully understand its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
Toxicological data for Triciribine phosphate sodium have been evaluated in preclinical studies, but detailed toxicity data are not extensively reported in the available literature. As an AKT inhibitor and purine biosynthesis inhibitor, potential toxicities could include myelosuppression, gastrointestinal effects, and metabolic disturbances. The compound is not approved for human use and is intended for research purposes only. Researchers should follow standard safety precautions when handling the compound, including working in a fume hood, wearing appropriate personal protective equipment, and avoiding inhalation, ingestion, or skin contact. The compound should be stored under nitrogen, away from moisture, at -20°C.
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| References | |
| Additional Infomation |
Triciribine phosphate sodium is a research-grade compound that functions as a potent, non-ATP competitive allosteric inhibitor of all three AKT isoforms (AKT1/PKBα, AKT2/PKBβ, AKT3/PKBγ). It also inhibits amidophosphoribosyltransferase and IMP dehydrogenase, affecting purine and guanosine nucleotide biosynthesis. The compound has been studied for its anticancer activity and has been evaluated in preclinical studies. It has the molecular formula C13H16N6NaO7P and a molecular weight of 422.27. Triciribine phosphate sodium (TCN-P sodium) has not been approved for any therapeutic indication but has been investigated in clinical trials as an anticancer agent. Its mechanism of action involves inhibition of AKT signaling and depletion of nucleotide pools, leading to antiproliferative and pro-apoptotic effects. The compound is available for research purposes and is not intended for human use.
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| Molecular Formula |
C13H16N6NAO7P
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| Molecular Weight |
422.27
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| Exact Mass |
422.071578
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| Related CAS # |
61966-08-3; 35943-35-2
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| Appearance |
White to light yellow solid powder
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| SMILES |
CN1C2=NC=NC3=C2C(=CN3[C@H]4[C@@H]([C@@H]([C@H](O4)COP(=O)(O)[O-])O)O)C(=N1)N.[Na+]
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| InChi Key |
ITOFBRQKZOZIJB-DOKXERMVSA-M
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| InChi Code |
InChI=1S/C13H17N6O7P.Na/c1-18-11-7-5(10(14)17-18)2-19(12(7)16-4-15-11)13-9(21)8(20)6(26-13)3-25-27(22,23)24;/h2,4,6,8-9,13,20-21H,3H2,1H3,(H2,14,17)(H2,22,23,24);/q;+1/p-1/t6-,8-,9-,13-;/m1./s1
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| Chemical Name |
Sodium [(2R,3S,4R,5R)-5-(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)-3,4-dihydroxyoxolan-2-yl]methyl hydrogen phosphate
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| Synonyms |
VQD-002 sodium; VQD 002 sodium; VQD002; Triciribine phosphate (sodium); TCN-P (sodium); PTX-200; PTX 200 sodium; PTX200; PTX-002 sodium; PTX002; PTX 002 sodium; NSC-280594 sodium; TCN-P; Triciribine phosphate;
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 :~62.5 mg/mL (~148.01 mM; with sonication (<60°C))
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3682 mL | 11.8408 mL | 23.6815 mL | |
| 5 mM | 0.4736 mL | 2.3682 mL | 4.7363 mL | |
| 10 mM | 0.2368 mL | 1.1841 mL | 2.3682 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.
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