5-Aza-4'-thio-2'-deoxycytidine
Based on 1 Customer Validation
5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd) is an orally active DNA methyltransferase I (DNMT1) inhibitor. 5-Aza-4'-thio-2'-deoxycytidine, a sulfur-containing deoxy-cytidine analog, has the potential for DNA hypomethylating and has antitumor effects.
For research use only. We do not sell to patients.
- Purity: 99.89%
- CAS No.: 169514-76-5
- Formula: C8H12N4O3S
- Molecular Weight:244.27
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
All DNA Methyltransferase Isoforms
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Biological Activity
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DNMT1 |
5-Aza-4'-thio-2'-deoxycytidine (5-Aza-T-dCyd; 72 h) inhibits leukemia lines: CCRF-CEM (IC50=0.2 μM), KG1a (IC50=0.06 μM). 5-Aza-4'-thio-2'-deoxycytidine also decreases viability in the NCI-H23 lung carcinoma (IC50=4.5 μM), HCT-116 colon carcinoma (IC50=58 μM) and IGROV-1 ovarian carcinoma (IC50=36 μM)[1].
5-Aza-4'-thio-2'-deoxycytidine (0.1-20 μM; 96 h) markedly depletes DNMT1 in NCI-H23 lung, HCT-116 colon and IGROV-1 ovarian cells. 5-Aza-4'-thio-2'-deoxycytidine (0.1, 0.5, 1 μM; 96 h) results in marked depletion of DNMT1 in CCRF-CEM and KG1a myeloid leukemia cells[1].
5-Aza-4'-thio-2'-deoxycytidine (1 μM; 96 h) induce CpG demethylation and re-expression of the p15 tumor suppressor gene[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H23 lung, HCT-116 colon and IGROV-1 ovarian cells
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Concentration:1, 5, 10, 20 μM
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Incubation Time:96 h
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Result:Markedly depleted DNMT1 in cells.
5-Aza-4'-thio-2'-deoxycytidine (5 mg/kg/day; IP; for 9 days) decreases DNMT1 levels in tumors of CCRF-CEM tumors mice xenografts[1].
5-Aza-4'-thio-2'-deoxycytidine (1.5 mg/kg; ip; QD×5 rest and repeat 3 cycles) provides modest suppression of tumor growth as well in the HCT116 colon carcinoma, OVCAR3 ovarian tumor xenograft model. 5-Aza-4'-thio-2'-deoxycytidine has minimal antitumor effect in the HL-60 leukemia xenografts[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Young female athymic nu/nu mice with NCI-H23 tumor fragment[1]
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Dosage:6.7 or 10 mg/kg
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Administration:IP; daily for 9 days
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Result:Had antitumor efficacy against NCI-H23 tumor xenografts.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 169514-76-5
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Appearance Solid
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Molecular Weight 244.27
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Formula C8H12N4O3S
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Color White to off-white
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SMILES
O[C@H]1C[C@H](N(C=N2)C(N=C2N)=O)S[C@@H]1CO
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Synonyms
5-Aza-T-dCyd; NTX-301
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (102.35 mM; ultrasonic and warming and heat to 60°C; 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. 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. 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)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Jaideep V Thottassery, et al. Novel DNA methyltransferase-1 (DNMT1) depleting anticancer nucleosides, 4'-thio-2'-deoxycytidine and 5-aza-4'-thio-2'-deoxycytidine. Cancer Chemother Pharmacol. 2014 Aug;74(2):291-302. [Content Brief]
[2]. Joel Morris, et al. F-aza-T-dCyd (NSC801845), a Novel Cytidine Analog, in Comparative Cell Culture and Xenograft Studies with the Clinical Candidates T-dCyd, F-T-dCyd, and Aza-T-dCyd. Mol Cancer Ther. 2021 Apr;20(4):625-631. [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. 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 | 4.0938 mL | 20.4692 mL | 40.9383 mL | 102.3458 mL |
| 5 mM | 0.8188 mL | 4.0938 mL | 8.1877 mL | 20.4692 mL | |
| 10 mM | 0.4094 mL | 2.0469 mL | 4.0938 mL | 10.2346 mL | |
| 15 mM | 0.2729 mL | 1.3646 mL | 2.7292 mL | 6.8231 mL | |
| 20 mM | 0.2047 mL | 1.0235 mL | 2.0469 mL | 5.1173 mL | |
| 25 mM | 0.1638 mL | 0.8188 mL | 1.6375 mL | 4.0938 mL | |
| 30 mM | 0.1365 mL | 0.6823 mL | 1.3646 mL | 3.4115 mL | |
| 40 mM | 0.1023 mL | 0.5117 mL | 1.0235 mL | 2.5586 mL | |
| 50 mM | 0.0819 mL | 0.4094 mL | 0.8188 mL | 2.0469 mL | |
| 60 mM | 0.0682 mL | 0.3412 mL | 0.6823 mL | 1.7058 mL | |
| 80 mM | 0.0512 mL | 0.2559 mL | 0.5117 mL | 1.2793 mL | |
| 100 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0235 mL |
5-Aza-4'-thio-2'-deoxycytidine Related Classifications
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