1. Epigenetics
  2. DNA Methyltransferase
  3. 5-Aza-4'-thio-2'-deoxycytidine

5-Aza-4'-thio-2'-deoxycytidine  (Synonyms: 5-Aza-T-dCyd; NTX-301)

Cat. No.: HY-139015 Purity: 99.09%
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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.

5-Aza-4'-thio-2'-deoxycytidine Chemical Structure

5-Aza-4'-thio-2'-deoxycytidine Chemical Structure

CAS No. : 169514-76-5

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50 mg USD 3680 In-stock
100 mg USD 5850 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target[1]

DNMT1

 

In Vitro

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.

Western Blot Analysis[1]

Cell Line: NCI-H23 lung, HCT-116 colon and IGROV-1 ovarian cells
Concentration: 1, 5, 10, 20 μM
Incubation Time: 96 h
Result: Markedly depleted DNMT1 in cells.
In Vivo

5-Aza-4'-thio-2'-deoxycytidine (6.7, 10 mg/kg/day; IP; for 9 days) is effective against NCI-H23 tumor xenografts[1].
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.

Animal Model: Young female athymic nu/nu mice with NCI-H23 tumor fragment[1]
Dosage: 6.7 or 10 mg/kg
Administration: IP; daily for 9 days
Result: Had antitumor efficacy against NCI-H23 tumor xenografts.
Molecular Weight

244.27

Formula

C8H12N4O3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1C[C@H](N(C=N2)C(N=C2N)=O)S[C@@H]1CO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0938 mL 20.4692 mL 40.9383 mL
5 mM 0.8188 mL 4.0938 mL 8.1877 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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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. 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
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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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Product Name:
5-Aza-4'-thio-2'-deoxycytidine
Cat. No.:
HY-139015
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