1404-15-5

• 常用中文名：诺拉霉素
• 常用英文名：Nogalamycin
• CAS号：1404-15-5
• 分子式：C₃₉H₄₉NO₁₆
• 分子量：787.80
• 相关类别： 信号通路 抗感染 细菌
• 发布时间：2018-08-23 20:49:32
• 更新时间：2024-01-09 20:24:13
• 诺加霉素是蒽环素类抗生素。诺加霉素是一种有效的抗革兰氏阳性菌抗生素,对某些肿瘤细胞也有细胞毒性。诺加拉霉素由诺加拉链霉菌诺加拉变种产生。诺加霉素在与DNA模板结合后选择性抑制RNA合成。诺加霉素可用于研究抗癌药物[1][2]。

名称

• 中文名: 诺拉霉素
• 英文名: nogalamycin
• 英文别名: antibiotic205t3; nogalomycin; NOGALAMYCIN; NOGALAMYCIN,STREPTOMYCES NOGALATER

物化性质

• 密度: 1.49g/cm3
• 沸点: 899.9ºC at 760mmHg
• 分子式: C₃₉H₄₉NO₁₆
• 分子量: 787.80
• 闪点: 498.1ºC
• 精确质量: 787.30500
• PSA: 229.44000
• LogP: 1.13800
• 外观性状: 固体
• 蒸汽压: 7.49E-35mmHg at 25°C
• 折射率: 1.648
• 储存条件: -20°C， 密封， 干燥

生物活性

• 描述: 诺加霉素是蒽环素类抗生素。诺加霉素是一种有效的抗革兰氏阳性菌抗生素,对某些肿瘤细胞也有细胞毒性。诺加拉霉素由诺加拉链霉菌诺加拉变种产生。诺加霉素在与DNA模板结合后选择性抑制RNA合成。诺加霉素可用于研究抗癌药物[1][2]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成
  信号通路 >> 抗感染 >> 细菌
• 靶点:

  RNA Synthesis[2]

• 体外研究: 诺加霉素(0-10μg/ml；2小时)对CHO、L1210和B16具有致死性,LD50分别为2.74μg/ml、0.25μg/ml和0.15μg/ml【1】。细胞毒性试验细胞系：CHO、L1210和B16细胞【1】浓度：0-10μg/ml孵育时间：2小时结果：LD50s分别为2.74μg/ml、0.25μg/ml和0.15μg/ml,对CHO、L1210和B16具有杀伤力。
• 体内研究: 诺加霉素(0-1000μg/kg；IP)可以逆转化学诱导的大鼠纤维肉瘤肿瘤和自发性肿瘤[3]。动物模型：大鼠【1】剂量：0-1000μg/kg给药：IP结果：化学诱导的大鼠纤维肉瘤肿瘤和自发性肿瘤消退,最有效浓度为556μg/kg。
• 参考文献:

  [1]. Bhuyan BK, et al. Cell kill kinetics of several nogalamycin analogs and adriamycin for Chinese hamster ovary, L1210 leukemia, and B16 melanoma cells in culture. Cancer Res. 1981;41(1):18-24.

  [2]. Bhuyan BK, et al. Differential interaction of nogalamycin with DNA of varying base composition. Proc Natl Acad Sci U S A. 1965;54(2):566-572.

  [3]. Bempong MA. Cytological effect of nogalamycin in mammals and regression of methylcholanthrene-induced and spontaneous tumors in rats. Int J Clin Pharmacol Biopharm. 1976;14(1):6-14.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : RA4550000 CHEMICAL NAME : Nogalamycin CAS REGISTRY NUMBER : 1404-15-5 LAST UPDATED : 199806 DATA ITEMS CITED : 22 MOLECULAR FORMULA : C39-H49-N-O16 MOLECULAR WEIGHT : 787.89 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 500 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 4600 ug/kg TOXIC EFFECTS : Gastrointestinal - hypermotility, diarrhea Gastrointestinal - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >300 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 13750 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 8500 ug/kg TOXIC EFFECTS : Skin and Appendages - other glands Nutritional and Gross Metabolic - weight loss or decreased weight gain TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 250 ug/kg TOXIC EFFECTS : Behavioral - muscle weakness Lungs, Thorax, or Respiration - acute pulmonary edema Lungs, Thorax, or Respiration - respiratory depression MUTATION DATA TYPE OF TEST : Mutation test systems - not otherwise specified TEST SYSTEM : Mammal - species unspecified Lymphocyte DOSE/DURATION : 12 umol/L REFERENCE : CBINA8 Chemico-Biological Interactions. (Elsevier Scientific Pub. Ireland Ltd., POB 85, Limerick, Ireland) V.1- 1969- Volume(issue)/page/year: 36,1,1981 *** REVIEWS *** TOXICOLOGY REVIEW CRTXB2 CRC Critical Reviews in Toxicology. (CRC Press, Inc., 2000 Corporate Blvd., NW, Boca Raton, FL 33431) V.1- 1971- Volume(issue)/page/year: 2,159,1973

安全

• 符号: GHS07, GHS08
• 信号词: Danger
• 危害声明: H302-H312-H332-H350-H360
• 警示性声明: P201-P280-P308 + P313
• 个人防护装备: Eyeshields;Faceshields;full-face particle respirator type N100 (US);Gloves;respirator cartridge type N100 (US);type P1 (EN143) respirator filter;type P3 (EN 143) respirator cartridges
• 危害码 (欧洲): T: Toxic;
• 风险声明 (欧洲): 45-46-61-20/21/22
• 安全声明 (欧洲): 53-22-36/37/39-45
• 危险品运输编码: NONH for all modes of transport
• RTECS号: RA4550000