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  3. Ancitabine hydrochloride

Ancitabine hydrochloride  (Synonyms: Cyclocytidine hydrochloride; Cyclo-CMP hydrochloride; Cyclo-C)

Cat. No.: HY-N0093 Purity: 99.83%
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Ancitabine hydrochloride is a cytarabine derivative that inhibits viral replication. Ancitabine hydrochloride blocks vaccinia virus DNA replication, the progression of viral protein synthesis from early to late stages, and one-step growth of vaccinia virus. Ancitabine hydrochloride is applicable to research related to vaccinia virus infection, leukemia, human cytomegalovirus infection and colorectal cancer.

For research use only. We do not sell to patients.

Ancitabine hydrochloride

Ancitabine hydrochloride Chemical Structure

CAS No. : 10212-25-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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200 mg In-stock
1 g In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Ancitabine hydrochloride is a cytarabine derivative that inhibits viral replication. Ancitabine hydrochloride blocks vaccinia virus DNA replication, the progression of viral protein synthesis from early to late stages, and one-step growth of vaccinia virus. Ancitabine hydrochloride is applicable to research related to vaccinia virus infection, leukemia, human cytomegalovirus infection and colorectal cancer[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HeLa ED50
0.05 μg/mL
Compound: 9, CycloC
Cytotoxicity against human HeLa cells after 48 hrs by Coulter counting analysis
Cytotoxicity against human HeLa cells after 48 hrs by Coulter counting analysis
[PMID: 178871]
HeLa ED50
0.06 μg/mL
Compound: cycloC
Cytotoxicity against human HeLa cells after 48 hrs by Coulter counting analysis
Cytotoxicity against human HeLa cells after 48 hrs by Coulter counting analysis
[PMID: 178872]
In Vitro

Ancitabine hydrochloride (10-11 μM; up to 48 h) non-toxically inhibits vaccinia virus replication in BSC40 African green monkey kidney cells with a 48-h IC99 of 11 μM, acting by blocking viral DNA replication and preventing progression from early to late viral protein synthesis[1].
Ancitabine hydrochloride (5 μg/mL; 2 days) completely inhibits replication of the KOS strain of HSV-1 in HEL cells at a concentration of 5 μg/mL maintained for 2 days[2].
Ancitabine hydrochloride (5 μg/mL; 2 days) completely inhibits replication of the Savage strain of HSV-2 in HEL cells at a concentration of 5 μg/mL maintained for 2 days, with activity slightly greater than that of Ara-A and Ara-T[2].
Ancitabine hydrochloride (0.14-10 μg/mL; 4 days) potently inhibits replication of the AD169 strain of HCMV in HEL cells, with an ED90 of 0.14 μg/mL and complete inhibition at 10 μg/mL maintained for 4 days[2].
Ancitabine hydrochloride (<0.010->100 μg/mL; 4 days) is non-toxic to stationary HEL cells at concentrations up to 100 μg/mL, but is highly cytotoxic to growing HEL cells with a CyD50 of <0.010 μg/mL, resulting in a low therapeutic index for growing cells of <0.071 and a high therapeutic index for stationary cells of >714 relative to its HCMV ED90 of 0.14 μg/mL[2].
Ancitabine hydrochloride (500 μM; 48 h) is converted to its triphosphate form in HCMV-infected HEL cells when treated with 500 μM of the agent for 48 hours, as detected by HPLC[2].
Ancitabine hydrochloride (5 μg/mL; 48 h) substantially suppresses synthesis of HCMV DNA in infected HEL cells when treated with 5 μg/mL of the agent for 48 hours[2].
Ancitabine hydrochloride (10 μM; 72 h) induces intracellular vesicle formation in human colorectal carcinoma HCT116 cells with reproducible morphological profiles[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[2]

Cell Line: human embryonic lung fibroblasts (HEL, stationary and growing)
Concentration: >100 μg/mL (stationary cells); <0.010 μg/mL (growing cells, CyD50)
Incubation Time: 4 days (replenished every other day)
Result: Showed no cytotoxicity to stationary HEL cells at concentrations up to 100 μg/mL.
Reduced viable growing HEL cell counts by 50% (CyD50) at <0.010 μg/mL.
Resulted in a therapeutic index (stationary cell CyD50 / HCMV ED90) of >714, while the therapeutic index (growing cell CyD50 / HCMV ED90) was <0.071.
In Vivo

Ancitabine hydrochloride is rapidly excreted in the urine of rhesus monkeys, Beagle dogs, and Sprague-Dawley rats[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

261.66

Formula

C9H12ClN3O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC[C@@H]1[C@@H](O)[C@H](OC2=N3)[C@H](N2C=CC3=N)O1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (191.09 mM)

DMSO : 25 mg/mL (95.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8218 mL 19.1088 mL 38.2175 mL
5 mM 0.7644 mL 3.8218 mL 7.6435 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 140 mg/mL (535.05 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 3.8218 mL 19.1088 mL 38.2175 mL 95.5438 mL
5 mM 0.7644 mL 3.8218 mL 7.6435 mL 19.1088 mL
10 mM 0.3822 mL 1.9109 mL 3.8218 mL 9.5544 mL
15 mM 0.2548 mL 1.2739 mL 2.5478 mL 6.3696 mL
20 mM 0.1911 mL 0.9554 mL 1.9109 mL 4.7772 mL
25 mM 0.1529 mL 0.7644 mL 1.5287 mL 3.8218 mL
30 mM 0.1274 mL 0.6370 mL 1.2739 mL 3.1848 mL
40 mM 0.0955 mL 0.4777 mL 0.9554 mL 2.3886 mL
50 mM 0.0764 mL 0.3822 mL 0.7644 mL 1.9109 mL
60 mM 0.0637 mL 0.3185 mL 0.6370 mL 1.5924 mL
80 mM 0.0478 mL 0.2389 mL 0.4777 mL 1.1943 mL
H2O 100 mM 0.0382 mL 0.1911 mL 0.3822 mL 0.9554 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Ancitabine hydrochloride
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