佐柔比星

佐柔比星用途

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]。

佐柔比星名称

[ CAS 号 ]:
54083-22-6

[ 中文名 ]:
佐柔比星

[ 英文名 ]:
Zorubicin

[中文别名 ]:

正定苯酰肼

[英文别名 ]:

Rubidazone
ZORUBICIN
Zorubicina [INN-Spanish]
zorubicine
Benzoylhydrazone daunorubicin
Zorubicin [INN]
daunomycin benzoylhydrazone
Zorubicine [INN-French]
Rubidazon
Zorubicinum [INN-Latin]

佐柔比星生物活性

[ 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。

佐柔比星物理化学性质

[ 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

佐柔比星毒性和生态

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)