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3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a novel and potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with anti-HIV effects. It inhibits XMRV with a CC50 of 43.5 μM in MCF-7 cells.
| ln Vitro |
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) was essentially inactive against Xenotropic Murine Leukemia-related Virus (XMRV) replication at a concentration of 100 μM in MCF-7 cells. [1]
In XMRV-infected MCF-7 cells, the EC50 and EC90 values for CS-92 were both >100 μM. The CC50 (cytotoxic concentration 50%) was 43.5 μM. [1] |
|---|---|
| Cell Assay |
The antiviral activity of CS-92 against XMRV was evaluated in cell culture using MCF-7 (breast cancer) and LNCaP (prostate cancer) cell lines.
Cells were grown to about 50% confluence, washed, and inoculated with XMRV at a multiplicity of infection (MOI) of approximately 3 in serum-free medium for 90 minutes at 37°C in the presence of 5% CO2. Following infection, cells were washed, detached, counted, and plated (1000 cells/well) in 96-well plates containing medium with the test compound at the desired concentration (ranging from 0.01 to 100 μM, in 10-fold increments, dissolved in DMSO or water based on solubility). Cellular morphology was monitored every 24 hours by microscopy for signs of toxicity. Cell viability was also quantified using an MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) colorimetric assay (referred to as CellTiter 96 AQueous One Solution assay in Methods) to determine cytotoxicity (CC50). Viral replication was assessed by measuring reverse transcriptase (RT) activity in the culture supernatant collected every 24 hours. The RT assay involved incubating viral supernatants with an oligo(dT)-poly(rA) primer-template, radiolabeled [α-32P]dTTP, and Mn2+ for 1 hour at 37°C. The incorporated radioactivity was captured on DEAE cellulose paper, washed, and quantified using a phosphor-imager. Inhibition of viral release (measured by RT activity) on day 6 post-inoculation was averaged over multiple experiments. The EC50 (median effective concentration) and EC90 (90% effective concentration) were determined from concentration-response curves using the median-effect method. [1] |
| Toxicity/Toxicokinetics |
In MCF-7 cells, the half-maximal cytotoxic concentration (CC50) of CS-92 was 43.5 μM, which represents the concentration at which cell viability decreased by 50%. [1]
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| References | |
| Additional Infomation |
3'-Azide-3'-deoxy-5-methylcytidine (CS-92) is a nucleoside analog included in a screening panel of 45 compounds (28 of which are FDA-approved) to evaluate its ability to inhibit the replication of heterophilic murine leukemia-associated virus (XMRV). XMRV is a retrovirus associated with prostate cancer and chronic fatigue syndrome. [1] It was classified as an HIV-1 nucleoside reverse transcriptase inhibitor (NRTI) tested against XMRV. [1] In this study, CS-92 did not show significant anti-XMRV activity at the tested concentrations. [1]
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| Molecular Formula |
C10H14N6O4
|
|---|---|
| Molecular Weight |
282.255960941315
|
| Exact Mass |
282.107
|
| CAS # |
1282040-14-5
|
| PubChem CID |
101644650
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| Appearance |
Light yellow to yellow solid powder
|
| LogP |
-1
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
20
|
| Complexity |
526
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
O[C@@H]1[C@@H]([C@@H](CO)O[C@H]1N1C=C(C)C(N)=NC1=O)N=[N+]=[N-]
|
| InChi Key |
HQIDXEHGLJUNPT-JXOAFFINSA-N
|
| InChi Code |
InChI=1S/C10H14N6O4/c1-4-2-16(10(19)13-8(4)11)9-7(18)6(14-15-12)5(3-17)20-9/h2,5-7,9,17-18H,3H2,1H3,(H2,11,13,19)/t5-,6-,7-,9-/m1/s1
|
| Chemical Name |
4-amino-1-[(2R,3R,4S,5S)-4-azido-3-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-methylpyrimidin-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) |
DMSO : ~83.33 mg/mL (~295.22 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5428 mL | 17.7142 mL | 35.4283 mL | |
| 5 mM | 0.7086 mL | 3.5428 mL | 7.0857 mL | |
| 10 mM | 0.3543 mL | 1.7714 mL | 3.5428 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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