54083-22-6

• 常用中文名：佐柔比星
• 常用英文名：Zorubicin
• CAS号：54083-22-6
• 分子式：C₃₄H₃₅N₃O₁₀
• 分子量：645.65600
• 相关类别： 信号通路 细胞周期/DNA损伤 DNA/RNA合成
• 发布时间：2018-08-13 11:29:22
• 更新时间：2026-07-02 10:49:43
• 柔比星(Rubidazon)是柔红霉素(HY-13062A)的衍生物。柔比星与拓扑异构酶II相互作用并抑制DNA聚合酶。柔比星可用于研究急性白血病和肉瘤[1][2][3][4][5]。

名称

• 中文名: 佐柔比星
• 英文名: N-[(E)-1-[(2S,4S)-4-(4-amino-5-hydroxy-6-methyloxan-2-yl)oxy-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-3,4-dihydro-1H-tetracen-2-yl]ethylideneamino]benzamide
• 中文别名: 正定苯酰肼
• 英文别名: zorubicine; Zorubicine [INN-French]; Rubidazon; Ccris; Benzoic acid, 1-(2S,4S)-4-(3-amino-2,3,6-trideoxy-.alpha.-L-lyxo-hexopyranosyl)oxy-1,2,3,4,6,11-hexahydro-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-2-naphthacenylethylidenehydrazide; Zorubicinum [INN-Latin]; Benzoic acid, 2-[1-[(2S,4S)-4-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-1,2,3,4,6,11-hexahydro-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-2-naphthacenyl]ethylidene]hydrazide; Benzoic acid, (1-(4-((3-amino-2,3,6-trideoxy-alpha,L-lyxo-hexopyranosyl)oxy)-1,2,3,4,6,11-hexahydro-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-2-naphthacenyl)ethylidene)hydrazide, (2S-cis); Zorubicin [inn]; Benzoic acid 2-[1-[(2S,4S)-4-[(3-amino-2,3,6-trideoxy-α-L-lyxo-hexopyranosyl)oxy]-1,2,3,4,6,11-hexahydro-2,5,12-trihydroxy-7-methoxy-6,11-dioxonaphthacen-2-yl]ethylidene] hydrazide; RUBIDAZON; N-[1-[(2S,4S)-4-(4-Amino-5-hydroxy-6-methyloxan-2-yl)oxy-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-3,4-dihydro-1H-tetracen-2-yl]ethylideneamino]benzamide; Zorubicina [INN-Spanish]; Rubidazone; ZORUBICIN; Zorubicin [INN]; Daunomycin benzoylhydrazone; Benzoylhydrazone daunorubicin; Rubidazone|||Rubidazone|||Rubidazon; daunomycin benzoylhydrazone; Brn

物化性质

• 密度: 1.54g/cm3
• 分子式: C₃₄H₃₅N₃O₁₀
• 分子量: 645.65600
• 精确质量: 645.23200
• PSA: 210.23000
• LogP: 3.33700
• 外观性状: 白色或近乎于白色结晶粉末

生物活性

• 描述: 柔比星(Rubidazon)是柔红霉素(HY-13062A)的衍生物。柔比星与拓扑异构酶II相互作用并抑制DNA聚合酶。柔比星可用于研究急性白血病和肉瘤[1][2][3][4][5]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶
  信号通路 >> 细胞周期/DNA损伤 >> DNA/RNA合成
• 体外研究: 柔比星(0.1-1μg/mL；0-24 h)影响细胞周期[2]。柔比星(0-128 nM/mL；20分钟)剂量依赖性地抑制DNA聚合酶α和β,并显示出对聚合酶的优先抑制[3]。细胞周期分析[2]。细胞系：人淋巴细胞系浓度：0.1-1μg/mL孵育时间：0-24小时结果：时间依赖性地增加了人淋巴细胞的G2积累,延迟了G1和G1-S过渡。导致G2期细胞逐步积累。
• 体内研究: 柔比星(12-18 mg/kg；肿瘤细胞注射后48小时腹腔注射)影响白血病集落形成单位[1]。Zorubicin(0.75-6.0 mg/kg；静脉注射)会增加麻醉比格犬的血浆组胺浓度,并产生即时低血压[3]。动物模型：具有P388肿瘤细胞的6至8周龄雄性DBA2小鼠[1]剂量：12-18 mg/kg给药：腹膜内注射；12-18毫克/千克；肿瘤细胞注射后48小时结果：显示白血病集落形成单位的D1/2值为1.6mg/kg。

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : DG3345000 CHEMICAL NAME : Benzoic acid, (1-(4-((3-amino-2,3,6-trideoxy-alpha,L-lyxo-hexopyran osyl)oxy)-1,2,3,4,6,1 1- hexahydro-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-2-na phthacenyl)ethylidene )hydrazide, (2S-cis)- CAS REGISTRY NUMBER : 54083-22-6 LAST UPDATED : 199703 DATA ITEMS CITED : 9 MOLECULAR FORMULA : C34-H35-N3-O10 MOLECULAR WEIGHT : 645.72 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Unreported SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 35 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 : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 22500 ug/kg/5D-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 : 75 mg/kg/5D-I TOXIC EFFECTS : Related to Chronic Data - death TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 42500 ug/kg/5D-I TOXIC EFFECTS : Related to Chronic Data - death MUTATION DATA TYPE OF TEST : DNA inhibition TEST SYSTEM : Rodent - rat Cells - not otherwise specified DOSE/DURATION : 2150 ug/L REFERENCE : BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1958- Volume(issue)/page/year: 38,167,1989 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X2089 No. of Facilities: 8 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 229 (estimated) No. of Female Employees: 82 (estimated)