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Ancitabine hydrochloride

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Catalog No. T1591Cas No. 10212-25-6
Alias NSC 145668 HCl, Cyclocytidine hydrochloride, Cyclocytidine HCl, Cyclo-CMP hydrochloride, Cyclo-C HCl

Ancitabine hydrochloride (NSC 145668 HCl) is the hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. Upon administration, ancitabine is slowly hydrolyzed into cytarabine. Subsequently, cytarabine is converted to the triphosphate form within the cell and then competes with cytidine for incorporation into DNA. Because the arabinose sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the S phase of the cell cycle. Cytarabine agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Compared to cytarabine, a more prolonged, consistent cytarabine-mediated therapeutic effect may be achieved with ancitabine because of the slow hydrolytic conversion of ancitabine to cytarabine.

Ancitabine hydrochloride

Ancitabine hydrochloride

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Purity: 99.37%
Catalog No. T1591Alias NSC 145668 HCl, Cyclocytidine hydrochloride, Cyclocytidine HCl, Cyclo-CMP hydrochloride, Cyclo-C HClCas No. 10212-25-6
Ancitabine hydrochloride (NSC 145668 HCl) is the hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. Upon administration, ancitabine is slowly hydrolyzed into cytarabine. Subsequently, cytarabine is converted to the triphosphate form within the cell and then competes with cytidine for incorporation into DNA. Because the arabinose sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the S phase of the cell cycle. Cytarabine agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Compared to cytarabine, a more prolonged, consistent cytarabine-mediated therapeutic effect may be achieved with ancitabine because of the slow hydrolytic conversion of ancitabine to cytarabine.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
500 mg$33-In Stock
1 g$42-In Stock
1 mL x 10 mM (in DMSO)$29In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.37%
Appearance:Solid
Color:White
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Product Introduction

Bioactivity
Description
Ancitabine hydrochloride (NSC 145668 HCl) is the hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. Upon administration, ancitabine is slowly hydrolyzed into cytarabine. Subsequently, cytarabine is converted to the triphosphate form within the cell and then competes with cytidine for incorporation into DNA. Because the arabinose sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the S phase of the cell cycle. Cytarabine agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Compared to cytarabine, a more prolonged, consistent cytarabine-mediated therapeutic effect may be achieved with ancitabine because of the slow hydrolytic conversion of ancitabine to cytarabine.
In vitro
Cyclocytidine, an effective immunosuppressant, antiviral, and antitumor agent, can be used in the treatment of leukemia. Its maximal inhibitory effect is achieved through administration via various composite injection methods.
In vivo
Cyclocytidine exhibits its most pronounced effects on cells that require DNA replication and are in the rapid division phase of mitosis. It inhibits DNA and RNA polymerases and nucleotide reductase, which are essential for DNA synthesis. Structurally similar to human deoxynucleosides, Cyclocytidine HCl (Ancitabine), integrates into human DNA, resulting in cell death. It serves as a prodrug of Cytarabine.
Kinase Assay
Human placental aromatase activity: The assay is performed in a total volume of 1 mL at 37 ℃. Unless otherwise noted, the incubation mixture contains 11 nM [4- 14C] androstene-3, 17-dione ([4- 14C]A), 24 mM NADPH (tetrasodium salt Type III), the appropriate concentrations of the desired inhibitor, and 120 μg of microsomal protein. The (4- 14C)A is added as a solution in 1.7% ethanol in 0.05 M potassium phosphate buffer (pH 7.4), so that the final concentration of ethanol does not exceed 0.02% (v/v). The reaction is started by the addition of enzyme and stopped after 20 min by the addition of 7 vol of ethyl acetate. The mixture is agitated on a vortex mixer and centrifuged at 600 g for 5 min. The aqueous phase is re-extracted with 7 vol of ethyl acetate, and the combined extracts are evaporated to dryness using an Evapo-Mix. Over 99% of the radio- active of [4- 14C] added is recovered using this extraction system. The residue obtained is dissolved in 150 μL acetone, and 100 μL aliquots are chromatographed for 65 min on thin-layer plates precoated with silica gel 60 using ethyl: acetate: isooctane (140:60, v/v; system A) or toluene: chloroform: methanol (70:140:20; system B). The radioactive zones of the plate are located with a Berthold LB 2760 thin-layer scanner. The radioactive estradiol (E2) and estrone (E1) neaks are identified by comparison with authentic standards. The corresponding bonding band of silica gel is transferred to vials containing 10 mL of scintillation fluid, and counted with a 6880 Liquid Scintillation system.
SynonymsNSC 145668 HCl, Cyclocytidine hydrochloride, Cyclocytidine HCl, Cyclo-CMP hydrochloride, Cyclo-C HCl
Chemical Properties
Molecular Weight261.66
FormulaC9H12ClN3O4
Cas No.10212-25-6
SmilesCl.[C@@H]12[C@@H](Oc3n1ccc(=N)n3)[C@@H]([C@H](O2)CO)O
Relative Density.2.01 g/cm3
Storage & Solubility Information
Storagestore under nitrogen | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 10 mg/mL (38.22 mM), Sonication is recommended.
H2O: 26.31 mg/mL (100.55 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (3.82 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO/H2O
1mg5mg10mg50mg
1 mM3.8218 mL19.1088 mL38.2175 mL191.0877 mL
5 mM0.7644 mL3.8218 mL7.6435 mL38.2175 mL
10 mM0.3822 mL1.9109 mL3.8218 mL19.1088 mL
20 mM0.1911 mL0.9554 mL1.9109 mL9.5544 mL
H2O
1mg5mg10mg50mg
50 mM0.0764 mL0.3822 mL0.7644 mL3.8218 mL
100 mM0.0382 mL0.1911 mL0.3822 mL1.9109 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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