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| Targets |
As a nucleoside analog, alpha-Cytidine targets the DNA synthesis machinery. It is incorporated into DNA during replication, where it likely acts as an antimetabolite. The anticancer mechanism of this class of compounds relies on the inhibition of DNA synthesis and induction of apoptosis (programmed cell death). Its specific binding partners are primarily the DNA polymerases involved in DNA replication.
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| ln Vitro |
In vitro, alpha-Cytidine serves as a chemical tool for studying the effects of nucleoside analogs on cell proliferation. Based on its classification as a purine nucleoside analog, it would inhibit the growth of various cancer cell lines by being incorporated into DNA, leading to chain termination and the induction of apoptosis. Its specific IC50 values for different cell lines are not provided in the summary.
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| ln Vivo |
In vivo, alpha-Cytidine is used for research related to life sciences. As a representative of its class, it is expected to exhibit antitumor activity by inhibiting DNA synthesis. However, detailed animal model studies for this specific alpha-isomer are not reported in the available literature. Its primary use is in mechanistic or cell-based studies exploring the pharmacological effects of nucleoside analogs.
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| Enzyme Assay |
Cell-free assays for alpha-Cytidine would likely involve DNA polymerase activity assays. In such a system, the compound can be tested as a substrate or inhibitor. For example, DNA polymerase and a DNA template are incubated with a mixture of natural deoxynucleotide triphosphates (dNTPs) and radio-labeled alpha-Cytidine. The incorporation of the analog into the nascent DNA strand can be measured by scintillation counting, and its effect on the rate of DNA synthesis can be assessed.
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| Cell Assay |
In cellular assays, cancer cell lines are cultured in 96-well plates and treated with varying concentrations of alpha-Cytidine (e.g., 0.1 uM to 100 uM) for 48-72 hours. Cell viability is measured using a luminescence-based CellTiter-Glo assay or a colorimetric MTT assay. Mechanistically, the induction of apoptosis can be assessed by staining cells with Annexin V and propidium iodide and analyzing them by flow cytometry.
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| Animal Protocol |
Specific in vivo animal study protocols for alpha-Cytidine are not provided in the literature. However, as a general protocol for nucleoside analogs, xenograft mouse models could be used. Immunocompromised mice bearing human tumor xenografts would be treated with alpha-Cytidine at specific doses (e.g., 25-100 mg/kg) administered via intraperitoneal (IP) injection daily. Tumor volume would be monitored with calipers to evaluate antitumor efficacy.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for alpha-Cytidine is not provided. The compound is water-soluble (≥ 50 mg/mL in H2O), which is typical for nucleosides. This high solubility would facilitate its absorption and distribution in vivo. Its structure suggests that it may be metabolized by similar pathways as natural nucleosides, potentially including deamination or phosphorylation by cellular kinases.
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| Toxicity/Toxicokinetics |
Toxicology data for alpha-Cytidine is not detailed in the summaries. As a nucleoside analog, it could potentially be incorporated into the DNA of both healthy and cancerous cells, which is the basis for both its antitumor activity and potential side effects. Its toxicity profile is likely the subject of ongoing research and is a key consideration for its use as an anticancer agent. No specific clinical data is reported.
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| References | |
| Additional Infomation |
alpha-Cytidine is primarily a tool compound for biochemical research to study structure-activity relationships, enzyme specificity (e.g., for nucleoside kinases or polymerases), and the behavior of nucleoside analogs in biological systems. It is not a drug candidate currently in clinical trials. Its value lies in its ability to help researchers understand the mechanism of action of the broader class of nucleoside analog drugs. It is a reference compound for analytical chemistry.
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| Molecular Formula |
C9H13N3O5
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|---|---|
| Molecular Weight |
243.22
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| Exact Mass |
243.086
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| CAS # |
13913-16-1
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| PubChem CID |
1265901
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| Appearance |
White to off-white solid powder
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| LogP |
-2.1
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
383
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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)CO)O)O
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| InChi Key |
UHDGCWIWMRVCDJ-JBBNEOJLSA-N
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| InChi Code |
InChI=1S/C9H13N3O5/c10-5-1-2-12(9(16)11-5)8-7(15)6(14)4(3-13)17-8/h1-2,4,6-8,13-15H,3H2,(H2,10,11,16)/t4-,6-,7-,8+/m1/s1
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| Chemical Name |
4-amino-1-[(2S,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 4.1115 mL | 20.5575 mL | 41.1150 mL | |
| 5 mM | 0.8223 mL | 4.1115 mL | 8.2230 mL | |
| 10 mM | 0.4112 mL | 2.0558 mL | 4.1115 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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