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| Targets |
Cytarabine triphosphate targets DNA polymerase and DNA synthesis. As a triphosphate nucleotide analog, it competes with deoxycytidine triphosphate (dCTP) for incorporation into growing DNA strands during replication. Once incorporated, the arabinose sugar moiety causes steric hindrance that prevents further DNA chain elongation, leading to chain termination and DNA strand breakage. This results in S-phase-specific cell death.
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| ln Vitro |
In vitro, Cytarabine triphosphate is the active metabolite responsible for the cytotoxic effects of cytarabine. It inhibits DNA polymerase activity and is incorporated into DNA, causing chain termination. The compound is used in cell-based assays to study the mechanisms of cytarabine resistance and to evaluate the activity of cytarabine analogs. Its potency is measured by IC50 values in various leukemia cell lines. The trisodium salt form enhances aqueous solubility for biochemical studies.
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| ln Vivo |
In vivo, Cytarabine triphosphate is formed intracellularly from cytarabine through sequential phosphorylation by deoxycytidine kinase and other nucleoside kinases. The active metabolite is responsible for the antitumor activity of cytarabine in the treatment of acute myeloid leukemia (AML) and other hematological malignancies. The compound itself is not administered as a drug but is studied to understand cytarabine pharmacology and resistance mechanisms.
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| Enzyme Assay |
Non-cellular enzyme assays for Cytarabine triphosphate involve measuring its inhibition of DNA polymerase activity. The compound is incubated with purified DNA polymerase, a DNA template, and competing dCTP. DNA synthesis is monitored by incorporating radiolabeled nucleotides or by using fluorescent detection methods. The compound's ability to inhibit DNA polymerase and be incorporated into DNA is assessed. These assays confirm the mechanism of action of cytarabine.
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| Cell Assay |
In vitro cellular experiments with Cytarabine triphosphate are limited due to the compound's poor cell permeability. However, cytarabine is used in cell-based assays, and its intracellular conversion to Ara-CTP is measured. Cells are treated with cytarabine, and Ara-CTP levels are quantified by HPLC or LC-MS/MS. The correlation between Ara-CTP accumulation and cytotoxicity is assessed. These studies are used to understand cytarabine resistance mechanisms.
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| Animal Protocol |
In vivo animal experiments with cytarabine involve administering the prodrug and measuring Ara-CTP levels in tissues. Tumor-bearing mice are treated with cytarabine, and the accumulation of Ara-CTP in tumor cells and normal tissues is measured. Pharmacodynamic studies correlate Ara-CTP levels with antitumor efficacy and toxicity. These studies are used to optimize dosing schedules and to evaluate new cytarabine formulations.
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| ADME/Pharmacokinetics |
Cytarabine triphosphate trisodium has a molecular weight of approximately 510.13 (trisodium salt). The compound is the active metabolite of cytarabine. It is typically stored at -20°C and protected from moisture. It is soluble in water and aqueous buffers. The compound is for research use only and is not intended for human therapeutic administration. Purity is typically ≥95%.
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| Toxicity/Toxicokinetics |
Toxicity data for Cytarabine triphosphate are related to the toxicity profile of cytarabine. The active metabolite causes myelosuppression, gastrointestinal toxicity, and other side effects associated with cytarabine therapy. As a research reagent, standard laboratory safety precautions should be followed when handling the compound. The compound is for research use only and not for human therapeutic applications.
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| References | |
| Additional Infomation |
Cytarabine triphosphate trisodium is also known as Ara-CTP trisodium. The CAS number is 1179343-17-9. The compound is the active metabolite of cytarabine (Ara-C), a standard chemotherapeutic agent for acute myeloid leukemia. It is used in research to study cytarabine pharmacology, resistance mechanisms, and to develop new nucleoside analogs. All products are for research use only.
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| Molecular Formula |
C9H13N3NA3O14P3
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|---|---|
| Molecular Weight |
549.10
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| Exact Mass |
548.93
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| CAS # |
1179343-17-9
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| PubChem CID |
169494469
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
32
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| Complexity |
875
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1=CN(C(=O)N=C1N)[C@H]2[C@H]([C@@H]([C@H](O2)COP(=O)([O-])OP(=O)([O-])OP(=O)(O)[O-])O)O.[Na+].[Na+].[Na+]
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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, 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) |
H2O :~125 mg/mL (~227.65 mM; with sonication)
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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 | 1.8212 mL | 9.1058 mL | 18.2116 mL | |
| 5 mM | 0.3642 mL | 1.8212 mL | 3.6423 mL | |
| 10 mM | 0.1821 mL | 0.9106 mL | 1.8212 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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