87081-35-4

• 常用中文名：来普霉素B
• 常用英文名：Leptomycin B
• CAS号：87081-35-4
• 分子式：C₃₃H₄₈O₆
• 分子量：540.73
• 相关类别： 原料药 抗生素类药物 其它抗生素类药
• 发布时间：2018-06-10 12:04:12
• 更新时间：2026-07-17 23:37:56
• Leptomycin B (CI 940; LMB) 是一种蛋白出核转运抑制剂。Leptomycin 通过半胱氨酸残基处的共价修饰使 CRM1/exportin 1 失活。 Leptomycin B 是一种有效的抗真菌抗生素,可阻断真核细胞周期。

名称

• 中文名: 来普霉素B
• 英文名: leptomycin B
• 中文别名: 立普拓素B; LTOMYCIN B (ETHANOL SOLUTION),ANTIBIOTIC,ANTIFUNGAL.抑制剂OF CRM-1 MEDIATED核EXPORT; 来普霉素B 溶液; LTOMYCIN B(LMB )来普霉素B; 细霉素B; 来普霉素B(出核转运抑制剂 0.2MG/ML); 乐托霉素B; 立普拓霉素B—莱普霉素B; 普霉素B杂质; 来普霉素B,10 MM DMSO 溶液; LTOMYCIN B 来普霉素B(出核转运抑制剂 0.2MG/ML); 来普霉素; 莱普霉素B; 立普拓霉素B; (2E,5S,6R,7S,9R,10E,12E,15R,16Z,18E)-17-乙基-6-羟基-3,5,7,9,11,15-六甲基-19-((2S,3S)-3-甲基-6-氧代-3,6-二氢-2H-吡喃-2-基)-8-氧杂代十九烷-2,10,12,16,18-戊酸; LTOMYCIN B (0.2MG/ML) 来普霉素B(出核转运抑制剂 0.2MG/ML)
• 英文别名: Ltomycin B solutio; Leptomycin B,(2E,5S,6R,7S,9R,10E,12E,15R,16Z,18E)-19-[(2S,3S)-3,6-Dihydro-3-methyl-6-oxo-2H-pyran-2-yl]-17-ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-8-oxo-2,10,12,16,18-nonadecapentaenoicacid; NSC 364372 CL 1957A Ltomycin B Antibiotic CI 940 Antibiotic CL 1957A; Ltomycin B (5 μg/mL in Ethanol); 2,10,12,16,18-nonadecapentanoicacid,19-(3,6-dihydro-3-methyl-6-oxo-2h-pyran-2; Elactocin, ATS 1287B, CI 940, CL 1957A, PD 114720, MantuaMycin; LTOMYCIN B; (2E,5S,6R,7S,9R,10E,12E,15R,16E,18E)-17-Ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-19-[(2S,3S)-3-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl]-8-oxo-2,10,12,16,18-nonadecapentaenoic acid; 2,10,12,16,18-Nonadecapentanoic acid, 19-(3,6-dihydro-3-methyl-6-oxo-2H-pyran-2-yl)-17-ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-8-oxo; LTOMYCIN B FROM STRTOMYCES SP; antibioticcl1957a; LEPTOMYCIN B FROM STREPTOMYCES SP; 2,10,12,16,18-Nonadecapentaenoicacid,19-[(2S,3S)-3,6-dihydro-3-methyl-6-oxo-2H-pyran-2-yl]-17-ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-8-oxo-,(2E,5S,6R,7S,9R,10E,12E,15R,16Z,18E); (2E,5S,6R,7S,9R,10E,12E,15R,16Z,18E)-19-[(2S,3S)-3,6-Dihydro-3-methyl-6-oxo-2H-pyran-2-yl]-17-ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-8-oxo-2,10,12,16,18-nonadecapentaenoicacid; Ltomycin B (ethanol solution), Antibiotic, antifungal. Inhibitor of CRM-1 mediated nucleexport; Lrimycin B; Ltomycin B (0.2mg/ml); CI-940, Elactocin, PD 114720, ATS 1287B, Mantuamycin, 19-(3,6-dihydro-3-methyl-6-oxo-2H-pyran-2-yl)-17-ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-8-oxo-2,10,12,16,18-Nonadecapentaenoic acid; (2E,10Z,12E,16Z,18E)-17-ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-19-(3-methyl-6-oxo-2,3-dihydropyran-2-yl)-8-oxo-nonadeca-2,10,12,16,18-pentaenoic acid; InSolution Ltomycin B; Ltomycin B, 10 mM in DMSO; Lomycin B; 2,10,12,16,18-nonadecapentaenoic acid; Ltomycin B (CI; LTOMYCIN B FROM STRTOMYCES SP //BP; antibioticci940; 2,10,12,16,18-Nonadecapentaenoic acid, 19-(3,6-dihydro-3-methyl-6-oxo-2H-pyran-2-yl)-17-ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-8-oxo; Ltomycin B solution from Strtomyces sp; XPO1,Chromosomal Maintenance 1,Fungal,inhibit,CI-940,EMT,Antibiotic,Ltomycin B,p53,nucleexport,mutation,EGFR,NSCLC,resistance,Inhibitor,CRM1,CI940,cancer,Exportin 1,KRAS; InSolution Ltomycin B, Strtomyces sp. - - Calbiochem; 7,9,11,15-hexamethyl-8-oxo-yl)-17-ethyl-6-hydroxy-5; 7,9,11,15-hexamethyl-8-oxo--yl)-17-ethyl-6-hydroxy-5; (2E,5S,6R,7S,9R,10E,12E,15R,16Z,18E)-17-Ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-19-((2S,3S)-3-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl)-8-oxononadeca-2,10,12,16,18-pentaenoic acid; LtoMycin B soluton; Ltomycin B, Strtomyces sp; (2E,5S,6R,7S,9R,10E,12E,15R,16Z,18E)-17-Ethyl-6-hydroxy-3,5,7,9,11,15-hexamethyl-19-[(2S,3S)-3-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl]-8-oxo-2,10,12,16,18-nonadecapentaenoic acid

物化性质

• 密度: 1.1±0.1 g/cm3
• 沸点: 725.8±60.0 °C at 760 mmHg
• 熔点: 41-44ºC
• 分子式: C₃₃H₄₈O₆
• 分子量: 540.73
• 闪点: 224.8±26.4 °C
• 精确质量: 540.345093
• PSA: 100.90000
• LogP: 6.66
• 外观性状: 白色结晶固体
• 蒸汽压: 0.0±5.3 mmHg at 25°C
• 折射率: 1.542

生物活性

• 描述: Leptomycin B (CI 940; LMB) 是一种蛋白出核转运抑制剂。Leptomycin 通过半胱氨酸残基处的共价修饰使 CRM1/exportin 1 失活。 Leptomycin B 是一种有效的抗真菌抗生素,可阻断真核细胞周期。
• 相关类别:
  研究领域 >> 癌症
  研究领域 >> 感染
  信号通路 >> 抗感染 >> 真菌
  信号通路 >> 跨膜转运 >> CRM1
• 靶点:

  CRM1/exportin 1[1]

• 参考文献:

  [1]. Kudo N, et al. Leptomycin B inactivates CRM1/exportin 1 by covalent modification at a cysteine residue in the central conserved region. Proc Natl Acad Sci U S A. 1999 Aug 3;96(16):9112-7.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : RA5390000 CHEMICAL NAME : 2,10,12,16,18-Nonadecapentanoic acid, 19-(3,6-dihydro-3-methyl-6-oxo-2H-pyran-2-yl)-17-ethy l- 6-hydroxy-3,5,7,9,11,15-hexamethyl-8-oxo- CAS REGISTRY NUMBER : 87081-35-4 LAST UPDATED : 199412 DATA ITEMS CITED : 3 MOLECULAR FORMULA : C33-H48-O6 MOLECULAR WEIGHT : 540.81 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 3100 ug/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value MUTATION DATA TYPE OF TEST : Mutation test systems - not otherwise specified TEST SYSTEM : Rodent - mouse Leukocyte DOSE/DURATION : 1 umol/L REFERENCE : PAACA3 Proceedings of the American Association for Cancer Research. (Waverly Press, 428 E. Preston St., Baltimore, MD 21202) V.1- 1954- Volume(issue)/page/year: 26,253,1985

安全

• 符号: GHS02, GHS06, GHS08
• 信号词: Danger
• 危害声明: H225-H301-H311-H331-H370
• 警示性声明: P210-P260-P280-P301 + P310-P311
• 危害码 (欧洲): T: Toxic;F: Flammable;
• 风险声明 (欧洲): R23/25
• 安全声明 (欧洲): 7-16-24-33-45
• 危险品运输编码: UN 1230 3
• WGK德国: 3
• 海关编码: 2916190090

合成路线

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海关

海关编码	2916190090
中文概述	2916190090 其他不饱和无环一元羧酸（包括其酸酐、酰卤化物，过氧化物和过氧酸以及它们的衍生物）。监管条件:AB(入境货物通关单,出境货物通关单)。增值税率:17.0%。退税率:9.0%。最惠国关税:6.5%。普通关税:30.0%
申报要素	品名, 成分含量, 用途, 丙烯酸、丙烯酸盐或酯应报明包装
监管条件	A.入境货物通关单 B.出境货物通关单
检验检疫	R.进口食品卫生监督检验 S.出口食品卫生监督检验 M.进口商品检验 N.出口商品检验
Summary	2916190090 unsaturated acyclic monocarboxylic acids, their anhydrides, halides, peroxides, peroxyacids and their derivatives。supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward)。VAT:17.0%。tax rebate rate:9.0%。MFN tariff:6.5%。general tariff:30.0%