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5-Aza-4＇-thio-2＇-deoxycytidine

CAS No. : 169514-76-5

MCE 站：5-Aza-4＇-thio-2＇-deoxycytidine

产品活性：5-Aza-4＇-thio-2＇-deoxycytidine (5-Aza-T-dCyd) 是一种口服有效的 DNA 甲基转移酶 I (DNMT1) 抑制剂。5-Aza-4＇-thio-2＇-deoxycytidine 是一种含硫脱氧胞苷类似物，具有 DNA 低甲基化的潜力。5-Aza-4＇-thio-2＇-deoxycytidine 具有抗肿瘤作用。

研究领域：Epigenetics

作用靶点：DNA Methyltransferase

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).
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.
5-Aza-4＇-thio-2＇-deoxycytidine (1 μM; 96 h) induce CpG demethylation ａnd re-expression of the p15 tumor suppressor gene.

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.
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.
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.

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