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Dihydro-5-azacytidine

Dihydro-5-azacytidine用途

核苷类似物二氢-5-氮杂胞苷(DHAC)被并入DNA并抑制DNA甲基化。二氢-5-氮杂胞苷具有抗肿瘤活性[1][2]。

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Dihydro-5-azacytidine名称

[ CAS 号 ]:
62488-57-7

[ 英文名 ]:
Dihydro-5-azacytidine

[英文别名 ]:

5,6 dihydro-5-azacytidine

Dihydro-5-azacytidine生物活性

[ 描述 ]:

核苷类似物二氢-5-氮杂胞苷(DHAC)被并入DNA并抑制DNA甲基化。二氢-5-氮杂胞苷具有抗肿瘤活性[1][2]。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> 核苷抗代谢药/类似物

信号通路 >> 表观遗传学 >> DNA甲基转移酶

[体外研究]

甲基化研究表明,与各自的对照组相比,LD10剂量的[3H]DHAC导致L1210/0细胞中的DNA低甲基化率为25.06%,脱氧胞苷激酶突变细胞系L1210/dCK(-)中的低甲基化率为46.32%[2]。二氢-5-氮杂胞苷(DHAC)与三磷酸胞苷竞争并入RNA,导致核糖体降解和蛋白质合成缺陷[1]。

[体内研究]

在荷瘤小鼠(注射L1210/0细胞)中,LD10剂量的二氢-5-氮杂胞苷(DHAC；1500 mg/kg)后,达到的血浆峰值浓度为317μM,双指数消除,t1/2α为1.03 h,t1/2β为5 h[2]。

[参考文献]

[1]. Robert A Kratzke, et al. Response to the methylation inhibitor dihydro-5-azacytidine in mesothelioma is not associated with methylation of p16INK4a: results of cancer and leukemia group B 159904. J Thorac Oncol. 2008 Apr;3(4):417-21.

[2]. W C Powell, et al. Biochemical pharmacology of 5,6-dihydro-5-azacytidine (DHAC) and DNA hypomethylation in tumor (L1210)-bearing mice. Cancer Chemother Pharmacol. 1988;21(2):117-21.

Dihydro-5-azacytidine物理化学性质

[ 密度 ]:
2.1±0.1 g/cm3

[ 沸点 ]:
529.1ºC at 760 mmHg

[ 分子式 ]:
C₈H₁₄N₄O₅

[ 分子量 ]:
246.221

[ 闪点 ]:
273.8ºC

[ 精确质量 ]:
246.096420

[ PSA ]:
140.64000

[ LogP ]:
-2.20

[ 折射率 ]:
1.823

Dihydro-5-azacytidine毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XZ3018500

CHEMICAL NAME :: s-Triazin-2(1H)-one, 5,6-dihydro-4-amino-1-beta-D-ribofuranosyl-

CAS REGISTRY NUMBER :: 62488-57-7

LAST UPDATED :: 199709

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C8-H14-N4-O5

MOLECULAR WEIGHT :: 246.26

WISWESSER LINE NOTATION :: T6NVN EN DHJ EZ C- BT5OTJ CQ DQ E1Q

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

TYPE OF TEST :: Mutation in mammalian somatic cells

TEST SYSTEM :: Rodent - mouse Embryo

DOSE/DURATION :: 30 umol/L

REFERENCE :: CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 42,817,1982