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依诺他滨

依诺他滨用途

Enocitabine 是一种核苷类似物,是一种有效的 DNA 复制 (DNA replication) 的抑制剂和 DNA 链终止剂。Enocitabine 可作为治疗急性骨髓性白血病和淋巴细胞性白血病的有效化疗药物。

依诺他滨名称

[ CAS 号 ]:
55726-47-1

[ 中文名 ]:
依诺他滨

[ 英文名 ]:
Enocitabine

[中文别名 ]:

山嵛阿糖啶

[英文别名 ]:

ENOCITABINE ANTINEOPLASTIC DRUGS
N(4)-Behenoyl-1-b-D-arabinofuranosylcytosine
BH-AC
n(sup4)-behenoylcytosinearabinoside
BEHENOYLCYTOSINE ARABINOSIDE
MFCD00866294
Enocitabine
Sunrabin
Enocitabine [INN:JAN]
N4-Behenoylcytosine arabinoside

依诺他滨生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 感染

信号通路 >> 细胞周期/DNA损伤 >> 核苷抗代谢药/类似物

信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成

信号通路 >> 抗感染 >> CMV

[ 靶点 ]

DNA replication[1]; CMV[3]

[体外研究]

依诺西他滨对脱氨基有抵抗力,因为依诺西他滨在阿糖胞苷部分的4-氨基位置上具有高度亲脂性基团[1]。吡柔比星和依诺西他滨联合应用对人宫颈癌HeLa S3细胞和人髓细胞白血病K562细胞的杀伤活性增强。依诺西他滨或依托泊苷对HeLa S3和K562细胞有协同作用[2]。在依诺西他滨存在下,在人巨细胞病毒(HCMV)感染细胞中检测到核苷类似物的三磷酸形式,HCMV DNA的合成受到强烈抑制[3]。

[参考文献]

[1]. Hamada A, et al. Clinical pharmacokinetics of cytarabine formulations.Clin Pharmacokinet. 2002;41(10):705-18.

[2]. Nagasawa M, et al.In vitro combined effects of pirarubicin (THP) and various antitumor drugs on human tumor cell lines. Gan To Kagaku Ryoho. 1990 Apr;17(4 Pt 1):633-8.

[3]. Nakamura K, et al. Antiviral effect of antileukemic drugs N4-behenoyl-1-beta-D-arabinofuranosylcytosine (BH-AC) and 2,2'-anhydro-1-beta-D-arabinofuranosylcytosine (cyclo-C) against human cytomegalovirus. J Med Virol. 1990 Jun;31(2):141-7.

依诺他滨物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 熔点 ]:
141-142ºC

[ 分子式 ]:
C₃₁H₅₅N₃O₆

[ 分子量 ]:
565.785

[ 精确质量 ]:
565.409058

[ PSA ]:
133.91000

[ LogP ]:
9.00

[ 折射率 ]:
1.554

[ 储存条件 ]:
-20°C Freezer

依诺他滨毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: JR1230400

CHEMICAL NAME :: Docosanamide, N-(1-beta-D-arabinofuranosyl-1,2-dihydro-2-oxo-4-pyri midinyl)-

CAS REGISTRY NUMBER :: 55726-47-1

LAST UPDATED :: 199612

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C31-H55-N3-O6

MOLECULAR WEIGHT :: 565.89

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1 gm/kg

TOXIC EFFECTS :: Blood - other changes

REFERENCE :: YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 25,691,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1100 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: GTKRDX Gan to Kagaku Ryoho. Cancer and Chemotherapy. (1-8-9 Yaesu, Chuo-ku, Tokyo 103, Japan) V.1- 1974- Volume(issue)/page/year: 10,2077,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1352 mg/kg

TOXIC EFFECTS :: Blood - other changes

REFERENCE :: YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 25,691,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 380 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 14,484,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1500 mg/kg

TOXIC EFFECTS :: Blood - other changes

REFERENCE :: YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 25,691,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 525 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 14,484,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 810 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: GTKRDX Gan to Kagaku Ryoho. Cancer and Chemotherapy. (1-8-9 Yaesu, Chuo-ku, Tokyo 103, Japan) V.1- 1974- Volume(issue)/page/year: 10,2077,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 14,484,1983

依诺他滨安全信息

[ 危害码 (欧洲) ]:
Xi