9-β-D-Arabinofuranosylguanine
Based on 1 Customer Validation
9-β-D-Arabinofuranosylguanine is a Guanosine (HY-N0097) analog and shows high affinity for deoxyguanosine kinase (dGK) with a Km of 8.0 μM. 9-β-D-Arabinofuranosylguanine can be used for the research of T-cell lymphoblastic disease.
For research use only. We do not sell to patients.
- Purity : 99.77%
- CAS No.: 38819-10-2
- Formula: C10H13N5O5
- Molecular Weight:283.24
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
Km: 8.0 μM (dGK)[2]
In Vitro
9-β-D-Arabinofuranosylguanine elicits cytotoxicity through the intracellular accumulation of its 5′-triphosphate, Ara-GTP, which inhibits DNA polymerase and ribonucleotide reductase and is incorporated into DNA, terminating DNA chain elongation, resulting in cell death[1][2].
9-β-D-Arabinofuranosylguanine is selectively toxic to cultured T-lymphoblasts due to their ability to accumulate higher levels of the cytotoxic metabolite, Ara-GTP, relative to B- and null lymphoblastoid cells[1].
9-β-D-Arabinofuranosylguanine (0-1000 μM; 72 h) shows cytotoxicity with IC50s of 4.2, 452 and 777 μM against MOLT-4, MOLT-4/Ara-G500 and MOLT-4/Ara-G900 cells, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MOLT-4 and Ara-G-resistant sublines: MOLT-4/Ara-G500 and MOLT-4/Ara-G900
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Concentration:0-1000 μM
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Incubation Time:72 h
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Result:Showed cytotoxicity with IC50s of 4.2, 452 and 777 μM against MOLT-4, MOLT-4/Ara-G500 and MOLT-4/Ara-G900 cells, respectively.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 38819-10-2
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Appearance Solid
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Molecular Weight 283.24
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Formula C10H13N5O5
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Color White to off-white
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SMILES
O=C1C2=C(N=C(N)N1)N([C@H]3[C@@H](O)[C@H](O)[C@@H](CO)O3)C=N2
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Synonyms
AraG
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro:
DMSO : 125 mg/mL (441.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Shewach DS, et al. Differential metabolism of 9-beta-D-arabinofuranosylguanine in human leukemic cells. Cancer Res. 1989 Dec 1;49(23):6498-502. [Content Brief]
[2]. Lotfi K, et al. Low level of mitochondrial deoxyguanosine kinase is the dominant factor in acquired resistance to 9-beta-D-arabinofuranosylguanine cytotoxicity. Biochem Biophys Res Commun. 2002 May 24;293(5):1489-96. [Content Brief]
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 (protect from light). 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 | 1 mM | 3.5305 mL | 17.6526 mL | 35.3053 mL | 88.2631 mL |
| 5 mM | 0.7061 mL | 3.5305 mL | 7.0611 mL | 17.6526 mL | |
| 10 mM | 0.3531 mL | 1.7653 mL | 3.5305 mL | 8.8263 mL | |
| 15 mM | 0.2354 mL | 1.1768 mL | 2.3537 mL | 5.8842 mL | |
| 20 mM | 0.1765 mL | 0.8826 mL | 1.7653 mL | 4.4132 mL | |
| 25 mM | 0.1412 mL | 0.7061 mL | 1.4122 mL | 3.5305 mL | |
| 30 mM | 0.1177 mL | 0.5884 mL | 1.1768 mL | 2.9421 mL | |
| 40 mM | 0.0883 mL | 0.4413 mL | 0.8826 mL | 2.2066 mL | |
| 50 mM | 0.0706 mL | 0.3531 mL | 0.7061 mL | 1.7653 mL | |
| 60 mM | 0.0588 mL | 0.2942 mL | 0.5884 mL | 1.4711 mL | |
| 80 mM | 0.0441 mL | 0.2207 mL | 0.4413 mL | 1.1033 mL | |
| 100 mM | 0.0353 mL | 0.1765 mL | 0.3531 mL | 0.8826 mL |
9-β-D-Arabinofuranosylguanine Related Classifications
HY-N0097A Related Classifications
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