11056-06-7

• 常用中文名：博莱霉素
• 常用英文名：Bleocin
• CAS号：11056-06-7
• 分子式：C₅₅H₈₅N₁₇O₂₅S₄
• 分子量：1415.551
• 相关类别： 研究领域 癌症
• 发布时间：2018-09-25 20:52:08
• 更新时间：2024-01-04 17:58:48
• 博莱霉素是一种糖肽抗生素。博莱霉素对一系列淋巴瘤、头颈癌和生殖细胞肿瘤具有强大的抗肿瘤活性。博莱霉素可用于癌症和化疗的研究[1][2][3][4]。

名称

• 中文名: 博来霉素
• 英文名: bleomycin A2
• 中文别名: 博莱霉素
• 英文别名: (3-{[(2'-{(5S,8S,9S,10R,13S)-15-{6-Amino-2-[(1S)-3-amino-1-{[(2S)-2,3-diamino-3-oxopropyl]amino}-3-oxopropyl]-5-methyl-4-pyrimidinyl}-13-[{[(2R,3S,4S,5S,6S)-3-{[(2R,3S,4S,5R,6R)-4-(carbamoyloxy)-3,5-dihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl]oxy}-4,5-dihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl]oxy}(1H-imidazol-5-yl)methyl]-9-hydroxy-5-[(1R)-1-hydroxyethyl]-8,10-dimethyl-4,7,12,15-tetraoxo-3,6,11,14-tetraazapentadec-1-yl}-2,; BLM; Bleomycin; bleomicin; BLEO; BLEOMYCIN SULPHATE; BLEXANE; Bleocin; Blenoxane

物化性质

• 分子式: C₅₅H₈₅N₁₇O₂₅S₄
• 分子量: 1415.551
• 精确质量: 1414.518433
• PSA: 794.66000
• 外观性状: 无色或淡黄色粉末
• 储存条件: 库房通风低温干燥

生物活性

• 描述: 博莱霉素是一种糖肽抗生素。博莱霉素对一系列淋巴瘤、头颈癌和生殖细胞肿瘤具有强大的抗肿瘤活性。博莱霉素可用于癌症和化疗的研究[1][2][3][4]。
• 相关类别:
  研究领域 >> 癌症
• 体外研究: 博莱霉素(0-4 mU/mL；1 h)诱导V79细胞的双链断裂[2]。博来霉素(0-1 mU/mL；1小时)可减少S期细胞DNA的迁移[2]。博莱霉素(0-3μg/mL；1小时)诱导G2细胞染色单体畸变[3]。
• 体内研究: 博莱霉素(1 mg和10μg；眶后窦注射一次)影响细胞有丝分裂,诱导肿瘤模型中的细胞凋亡[4]。动物模型：LPB和B16F0肿瘤C57Bl/6小鼠[4]剂量：1mg和10μg给药：眶后窦注射；1 mg和10μg一次。结果：两种肿瘤中有丝分裂的细胞比例降低,电脉冲传递后诱导细胞凋亡,LPB肿瘤中非典型细胞数量增加。
• 参考文献:

  [1]. Chen J, Stubbe J. Bleomycins: towards better therapeutics. Nat Rev Cancer. 2005;5(2):102-112.

  [2]. Olive PL, et al. Detection of DNA double-strand breaks through the cell cycle after exposure to X-rays, bleomycin, etoposide and 125IdUrd. Int J Radiat Biol. 1993 Oct;64(4):349-58.

  [3]. Allio T, Preston RJ. Increased sensitivity to chromatid aberration induction by bleomycin and neocarzinostatin results from alterations in a DNA damage response pathway. Mutat Res. 2000 Sep 20;453(1):5-15.

  [4]. Mekid H, et al. In vivo evolution of tumour cells after the generation of double-strand DNA breaks. Br J Cancer. 2003 Jun 2;88(11):1763-71.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : EC5988000 CHEMICAL NAME : Bleomycin CAS REGISTRY NUMBER : 11056-06-7 LAST UPDATED : 199706 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : Standard Draize test ROUTE OF EXPOSURE : Administration into the eye SPECIES OBSERVED : Rodent - rabbit TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Human DOSE/DURATION : 351 mg/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - fibrosing alveolitis Lungs, Thorax, or Respiration - dyspnea TYPE OF TEST : LDLo - Lowest published lethal dose ROUTE OF EXPOSURE : Intramuscular SPECIES OBSERVED : Human DOSE/DURATION : 418 mg/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - fibrosing alveolitis Lungs, Thorax, or Respiration - dyspnea TYPE OF TEST : LD - Lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : >200 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 - rat DOSE/DURATION : 168 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 : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 168 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 : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >2 gm/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 : 35 mg/kg TOXIC EFFECTS : Tumorigenic - active as anti-cancer agent TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 188 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 : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 53 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 : Intramuscular SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 270 mg/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 : Intratracheal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 14 mg/kg TOXIC EFFECTS : Nutritional and Gross Metabolic - weight loss or decreased weight gain TYPE OF TEST : LD - Lethal dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Mammal - dog DOSE/DURATION : >100 mg/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 158 mg/kg/5W-I TOXIC EFFECTS : Lungs, Thorax, or Respiration - other changes TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 88200 ug/kg/9D-I TOXIC EFFECTS : Related to Chronic Data - death TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 40 mg/kg/4W-I TOXIC EFFECTS : Lungs, Thorax, or Respiration - other changes TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 160 mg/kg/4W-I TOXIC EFFECTS : Behavioral - food intake (animal) Lungs, Thorax, or Respiration - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 6875 ug/kg/41D-I TOXIC EFFECTS : Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair Skin and Appendages - nails TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Mammal - dog DOSE/DURATION : 11 mg/kg/41D-I TOXIC EFFECTS : Skin and Appendages - dermatitis, other (after systemic exposure) Skin and Appendages - hair Skin and Appendages - nails TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Primate - monkey DOSE/DURATION : 44 mg/kg/30D-I TOXIC EFFECTS : Cardiac - cardiomyopathy including infarction Kidney, Ureter, Bladder - changes primarily in glomeruli Skin and Appendages - dermatitis, other (after systemic exposure) TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intraperitoneal DOSE : 200 mg/kg SEX/DURATION : male 1 day(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) TYPE OF TEST : Specific locus test TYPE OF TEST : Sex chromosome loss and nondisjunction TYPE OF TEST : Cytogenetic analysis TYPE OF TEST : DNA damage TYPE OF TEST : Sex chromosome loss and nondisjunction TYPE OF TEST : Mutation test systems - not otherwise specified TYPE OF TEST : DNA inhibition TYPE OF TEST : Cytogenetic analysis TYPE OF TEST : Sister chromatid exchange TYPE OF TEST : Micronucleus test TYPE OF TEST : Micronucleus test TYPE OF TEST : Cytogenetic analysis TYPE OF TEST : Cytogenetic analysis TYPE OF TEST : Sister chromatid exchange TYPE OF TEST : DNA inhibition MUTATION DATA TYPE OF TEST : Cytogenetic analysis TEST SYSTEM : Mammal - cattle Sperm DOSE/DURATION : 100 mg/L REFERENCE : MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 326,185,1995 *** REVIEWS *** IARC Cancer Review:Animal Limited Evidence IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,134,1987 IARC Cancer Review:Human Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 26,97,1981 IARC Cancer Review:Group 2B IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,134,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4340 No. of Facilities: 356 (estimated) No. of Industries: 1 No. of Occupations: 8 No. of Employees: 8140 (estimated) No. of Female Employees: 5555 (estimated)

安全

• 危害码 (欧洲): T: Toxic;
• 风险声明 (欧洲): 46-40
• 安全声明 (欧洲): 53-36/37-45
• WGK德国: 3
• RTECS号: EC5991990