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Decitabine

CAS No. : 2353-33-5

MCE 国际站：Decitabine

产品活性：Decitabine (5-Aza-2'-deoxycytidine) 是一种具有口服活性的脱氧胞苷类似物抗代谢物 (deoxycytidine analogue antimetabolite) 和 DNA 甲基转移酶 (DNA methyltransferase) 抑制剂。Decitabine 代替 DNA 掺入胞嘧啶可以将 DNA 甲基转移酶共价捕获到 DNA 中，从而导致对该酶的不可逆抑制。Decitabine 诱导细胞 G2/M 阻滞和细胞凋亡 (apoptosis)，并具有有效的抗癌活性。

研究领域：Epigenetics  |  Apoptosis  |  Cell Cycle/DNA Damage

作用靶点：DNA Methyltransferase  |  Apoptosis  |  Nucleoside Antimetabolite/Analog

In Vitro: Decitabine treatment significantly inhibits cell growth of SNU719, NCC24 and KATOIII 96 hours after exposure to decitabine. Decitabine induces G2/M arrest and apoptosis in EBVaGC, inhibits invasion ability, and up-regulates E-cadherin expression for EBVaGC.
?Only high concentrations (10 μM) Decitabine (0.1-1 μM; 24-72 hours) results in a G2 phase arrest, which is accompanied by a reduction of cells in G1 phase.
?Decitabine up-regulates DCTPP1 and dUTPase expression in HeLa cells.

In Vivo: Decitabine (1.0 mg/kg, p.o.) in combination with tetrahydrouridine (THU) causes severe toxicity occurs in female CD-1 mice, and results in an increased sensitivity to decitabine toxicity correlating with decitabine plasma levels.
?Decitabine (1.0 mg/kg; i.p.; once daily for 5 consecutive days) leads to regression of EL4 tumors established in C57BL/6 Mice.

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