169514-76-5
169514-76-5 structure
- Name: 5-Aza-4'-thio-2'-deoxycytidine
- Chemical Name: 5-Aza-4'-thio-2'-deoxycytidine
- CAS Number: 169514-76-5
- Molecular Formula: C8H12N4O3S
- Molecular Weight: 244.27
- Catalog: Signaling Pathways Epigenetics DNA Methyltransferase
- Create Date: 2021-09-05 10:24:37
- Modify Date: 2024-01-03 08:24:56
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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[1].
| Name | 5-Aza-4'-thio-2'-deoxycytidine |
|---|
| 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]. |
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| Related Catalog | |
| Target |
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]. 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]. 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. |
| References |
| Molecular Formula | C8H12N4O3S |
|---|---|
| Molecular Weight | 244.27 |