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二溴甘露醇

二溴甘露醇用途

米托溴醇(Myelobromol；DBM)是甘露醇的溴化类似物,也被称为一种被归类为烷基化剂的抗癌剂。丝裂霉素具有骨髓抑制的潜力,与加速慢性粒细胞白血病中异基因骨髓移植的几种并发症风险显著降低相关[1][2]。

二溴甘露醇名称

[ CAS 号 ]:
488-41-5

[ 中文名 ]:
二溴甘露醇

[ 英文名 ]:
1,6-DIBROMO-1,6-DIDEOXY-D-MANNITOL

[中文别名 ]:

1,6-二溴-1,6-二脱氧-D-甘露糖醇

[英文别名 ]:

r54
1.6-dibromo-1.6-dideoxy-D-mannitol
1,6-dibromo-D-1,6-dideoxy-mannitol
1.6-Dibrom-1.6-didesoxy-D-mannit
dibromannit
dibromomannitol
EINECS 207-676-8
Mielobromol
mieobromol
myelobromol

二溴甘露醇生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> DNA烷基化剂/交联剂

[体内研究]

在小鼠模型中,丝裂霉素(850 mg/kg；i.p.；单剂量)提高脾细胞对有丝分裂原的敏感性,并促进胸腺再生[2]。动物模型：雌性BALB/c小鼠(8-10周龄)[2]剂量：850 mg/kg；1500 mg/kg(悬浮于5%吐温80盐水中,0.5 mL)给药：腹膜内注射；单剂量结果：850mg/kg剂量对脾细胞对有丝分裂原的体外增殖反应有影响。在1500 mg/kg剂量下,胸腺再生增强,比对照早,开始恢复时间为2周,次全恢复时间为3周。

二溴甘露醇物理化学性质

[ 密度 ]:
2.117g/cm3

[ 沸点 ]:
511.2ºC at 760mmHg

[ 熔点 ]:
176-178°

[ 分子式 ]:
C₆H₁₂Br₂O₄

[ 分子量 ]:
307.96500

[ 闪点 ]:
263ºC

[ 精确质量 ]:
305.91000

[ PSA ]:
80.92000

[ 蒸汽压 ]:
1.37E-12mmHg at 25°C

[ 折射率 ]:
1.622

[ 储存条件 ]:
−20°C

二溴甘露醇毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: OP2800000

CHEMICAL NAME :: Mannitol, 1,6-dibromo-1,6-dideoxy-, D-

CAS REGISTRY NUMBER :: 488-41-5

BEILSTEIN REFERENCE NO. :: 1721919

LAST UPDATED :: 199707

DATA ITEMS CITED :: 36

MOLECULAR FORMULA :: C6-H12-Br2-O4

MOLECULAR WEIGHT :: 308.00

WISWESSER LINE NOTATION :: E1YQYQYQYQ1E

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1500 mg/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - other changes Blood - normocytic anemia

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 900 mg/kg

TOXIC EFFECTS :: Blood - normocytic anemia Blood - thrombocytopenia

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1240 mg/kg

TOXIC EFFECTS :: Gastrointestinal - hypermotility, diarrhea Gastrointestinal - other changes Blood - normocytic anemia

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1370 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 :: 1380 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - ataxia Skin and Appendages - hair

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 900 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - ataxia Skin and Appendages - hair

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2200 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - ataxia Skin and Appendages - hair

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2200 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 - rabbit

DOSE/DURATION :: 1080 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 :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4950 mg/kg/33D-I

TOXIC EFFECTS :: Behavioral - ataxia Liver - other changes Blood - changes in leukocyte (WBC) count

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 5460 mg/kg/26W-I

TOXIC EFFECTS :: Endocrine - changes in thymus weight Blood - normocytic anemia Related to Chronic Data - death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 10920 mg/kg/26W-C

TOXIC EFFECTS :: Related to Chronic Data - changes in testicular weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9750 mg/kg/26W-I

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Skin and Appendages - tumors Tumorigenic - tumors at site of application

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7000 mg/kg/26W-I

TOXIC EFFECTS :: Tumorigenic - neoplastic by RTECS criteria Lungs, Thorax, or Respiration - tumors Blood - lymphoma, including Hodgkin's disease

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 300 mg/kg

SEX/DURATION :: female 9-14 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3900 mg/kg

SEX/DURATION :: female 26 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Maternal Effects - ovaries, fallopian tubes Reproductive - Maternal Effects - uterus, cervix, vagina

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 500 mg/kg

SEX/DURATION :: female 13 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 500 mg/kg

SEX/DURATION :: female 10 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - urogenital system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 300 mg/kg

SEX/DURATION :: female 9 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3900 mg/kg

SEX/DURATION :: male 26 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 150 mg/kg

SEX/DURATION :: female 11 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Embryo or Fetus - fetal death

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 150 mg/kg

SEX/DURATION :: female 11 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - musculoskeletal system

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 300 mg/kg

SEX/DURATION :: female 12 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - Central Nervous System Reproductive - Specific Developmental Abnormalities - eye/ear

TYPE OF TEST :: Sex chromosome loss and nondisjunction

TYPE OF TEST :: Heritable translocation test

TYPE OF TEST :: Cytogenetic analysis

TYPE OF TEST :: Sister chromatid exchange

MUTATION DATA

TYPE OF TEST :: DNA inhibition

TEST SYSTEM :: Rodent - rabbit Bone marrow

DOSE/DURATION :: 730 umol/L

REFERENCE :: BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1958- Volume(issue)/page/year: 25,1705,1976 *** 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: 1(1),93,1971 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

二溴甘露醇安全信息

[ 危害码 (欧洲) ]:
T: Toxic;

[ 风险声明 (欧洲) ]:
45-22

[ 安全声明 (欧洲) ]:
S22;S45;S53;S36/S37/S39

[ WGK德国 ]:
3

[ RTECS号 ]:
OP2800000

[ 海关编码 ]:
2905590090

二溴甘露醇合成路线

详细合成路线

二溴甘露醇制备

由D-甘露醇与氢溴酸反应得到二溴甘露醇:
将甘露醇溶解于氢溴酸,加热回流3h。加水稀释并降温至52℃,加入活性炭脱色。过滤,将滤液降温至20℃,搅拌下用碳酸氢钠调节pH1~2,冷冻后甩滤、水洗、氯仿洗涤,真空干燥后用甲醇重结晶、活性炭脱色精制而得成品。收率约36%。

二溴甘露醇海关

[ 海关编码 ]: 2905590090

[ 中文概述 ]:
2905590090 其他无环醇的卤化、磺化等衍生物。监管条件:无。增值税率:17.0%。退税率:9.0%。最惠国关税:5.5%。普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2905590090 other halogenated, sulphonated, nitrated or nitrosated derivatives of acyclic alcohols。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:5.5%。General tariff:30.0%