55726-47-1

• 常用中文名：依诺他滨
• 常用英文名：Enocitabine
• CAS号：55726-47-1
• 分子式：C₃₁H₅₅N₃O₆
• 分子量：565.785
• 相关类别： 信号通路 抗感染 CMV
• 发布时间：2018-03-13 08:00:00
• 更新时间：2024-01-04 22:49:22
• 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。

名称

• 中文名: 依诺他滨
• 英文名: Enocitabine
• 中文别名: N-[1-[3,4-二羟基-5-(羟甲基)氧杂环戊-2-基]-2-氧代嘧啶-4-基]山嵛酸酰胺; 山嵛阿糖啶
• 英文别名: 1-(β-D-Arabinofuranosyl)-4-(docosanoylamino)pyrimidin-2(1H)-one; ENOCITABINE ANTINEOPLASTIC DRUGS; N(4)-Behenoyl-1-b-D-arabinofuranosylcytosine; BH-AC; n(sup4)-behenoylcytosinearabinoside; 1-(β-D-Arabinofuranosyl)-4-(docosanoylamino)-2(1H)-pyrimidinone; BEHENOYLCYTOSINE ARABINOSIDE; MFCD00866294; Docosanamide, N-(1-β-D-arabinofuranosyl-1,2-dihydro-2-oxo-4-pyrimidinyl)-; Enocitabine; Sunrabin; 2(1H)-Pyrimidinone, 1-β-D-arabinofuranosyl-4-[(1-oxodocosyl)amino]-; N-(1-b-D-Arabinofuranosyl-1,2-dihydro-2-oxo-4-pyrimidinyl)docosanamide; Enocitabine [INN:JAN]; N4-Behenoylcytosine arabinoside

物化性质

• 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

生物活性

• 描述: 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。
• 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.

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

安全

• 危害码 (欧洲): Xi