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盐酸环胞苷

盐酸环胞苷用途

【用途1】
生产滴眼液。
【用途2】
抗肿瘤药。不良反应和阿糖胞苷相似,但较轻。有骨髓抑制作用。白细胞、血小板减少。用量大时常出现腮腺痛,局部冷敷可使疼痛减轻。有时可见流涎,有时可见体位性低血压、结膜充血、鼻黏膜肿胀,个别病人出现头痛、皮疹,偶可引起一过性肺部炎症变化。用药期间应严格检查血象。
【用途3】
对各种类型急性白血病及脑膜白血病均有效
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盐酸环胞苷名称

[ CAS 号 ]:
10212-25-6

[ 中文名 ]:
盐酸环胞苷

[ 英文名 ]:
Cyclocytidine Hydrochloride

[中文别名 ]:

[英文别名 ]:

盐酸环胞苷生物活性

盐酸环胞苷物理化学性质

[ 密度 ]:
2.01 g/cm3

[ 沸点 ]:
442ºC at 760 mmHg

[ 熔点 ]:
269-270ºC

[ 分子式 ]:
C9H12ClN3O4

[ 分子量 ]:
261.662

[ 闪点 ]:
221.1ºC

[ 精确质量 ]:
261.051636

[ PSA ]:
100.59000

[ 外观性状 ]:
白色固体

[ 折射率 ]:
-21 ° (C=2, H2O)

[ 储存条件 ]:
室温,干燥,密封

盐酸环胞苷MSDS

盐酸环胞苷毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
LV2615000
CAS REGISTRY NUMBER :
10212-25-6
LAST UPDATED :
199512
DATA ITEMS CITED :
21
MOLECULAR FORMULA :
C9-H11-N3-O4.Cl-H
MOLECULAR WEIGHT :
261.69
WISWESSER LINE NOTATION :
T B555 AN CO GO IN JHTT&J D1Q EQ &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
120 mg/kg
TOXIC EFFECTS :
Vascular - BP lowering not characterized in autonomic section Gastrointestinal - nausea or vomiting Blood - changes in bone marrow (not otherwise specified)
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>7 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 - rat
DOSE/DURATION :
3800 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 :
>5500 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 - rat
DOSE/DURATION :
820 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 :
>7 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 :
2528 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 - mouse
DOSE/DURATION :
4050 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 :
800 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 :
Mammal - dog
DOSE/DURATION :
344 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
1045 mg/kg
TOXIC EFFECTS :
Behavioral - changes in motor activity (specific assay) Gastrointestinal - changes in structure or function of salivary glands Gastrointestinal - nausea or vomiting
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
560 mg/kg/7D-I
TOXIC EFFECTS :
Blood - changes in leukocyte (WBC) count Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
1120 mg/kg/7D-I
TOXIC EFFECTS :
Behavioral - food intake (animal) Blood - changes in leukocyte (WBC) count Related to Chronic Data - death
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
400 mg/kg
SEX/DURATION :
female 8-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
800 mg/kg
SEX/DURATION :
female 8-15 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
8250 mg/kg
SEX/DURATION :
male 2 year(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 :
Intravenous
DOSE :
60 mg/kg
SEX/DURATION :
female 8-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - eye/ear Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
DOSE :
60 mg/kg
SEX/DURATION :
female 8-17 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 :
Intravenous
DOSE :
125 mg/kg
SEX/DURATION :
female 8-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - body wall

MUTATION DATA

TYPE OF TEST :
DNA inhibition
TEST SYSTEM :
Rodent - mouse Leukocyte
DOSE/DURATION :
10 mg/L
REFERENCE :
CPBTAL Chemical and Pharmaceutical Bulletin. (Japan Pub. Trading Co., USA, 1255 Howard St., San Francisco, CA 94103) V.6- 1958- Volume(issue)/page/year: 20,2286,1972
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盐酸环胞苷安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 安全声明 (欧洲) ]:
S24/25

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
2

[ RTECS号 ]:
LV2615000

盐酸环胞苷上下游产品

盐酸环胞苷上游产品

盐酸环胞苷下游产品

盐酸环胞苷制备

【方法1】
以葡萄糖酸钙为原料
D-阿拉伯糖的制备 投料为葡萄糖酸钙(m):水(V):过氧化氢(30%,V):葡萄糖酸铁水溶液(10%,V):95%乙醇(V)=1:8.1:0.88:0.22:0.3。将葡萄糖酸钙投入90℃水中,加热至沸腾。搅拌10min后降温至70℃,加入葡萄糖酸铁。搅拌10min后降温至65℃,每隔20min加一次过氧化氢,6h内加完,其间保持温度为60-65℃。反应完成后冷却,过滤,将滤液通过强酸性苯乙烯系阳离子交换树脂007×7(732)和强碱性季铵I型阴离子交换树脂201×7(717),当流出液对斐林试液呈阳性反应时开始收集。收集液于60℃以下减压浓缩,加95%乙醇,放置过夜,过滤,干燥,得产品。
葡萄糖酸钙[葡萄糖酸铁,过氧化氢]→[60-65℃, 6h]D-阿拉伯糖
2-氨基-β-D-阿拉伯糖噁唑啉的制备 投料比为D-阿拉伯糖(m):氰胺(V):25%-28%氨水(V):甲醇(V)=1:0.29:0.5:3。将D-阿拉伯糖、氰胺、甲醇-氨水溶液加热,于40-45℃反应4h,冷却过夜后过滤,得产品。
D-阿拉伯糖[氰胺,氨水,甲醇]→[40-45℃, 4h]2-氨基-β-D-阿拉伯糖噁唑啉
环胞苷盐酸盐的制备 投料体积比为2-氨基-β-D-阿拉伯糖噁唑啉(V):丙炔氰:5%盐酸甲醇溶液=1:0.59:4.83。将2-氨基-β-D-阿拉伯糖噁唑啉加5%盐酸甲醇溶液成盐酸盐后,加丙炔氰于60℃反应1h,冷却,抽滤,得粗品。用3倍量的水-95%乙醇(1:2.5)重结晶,得环胞苷盐酸盐纯品。
2-氨基-β-D-阿拉伯糖噁唑啉[丙炔氰,盐酸-甲醇]→[60℃, 1h]环胞苷盐酸盐。
【方法2】
D-阿拉伯糖与氰氨、甲醇、氨水在40-45℃反应4小时,生成2-氨基-β-D-阿拉伯糖噁唑啉,将其与盐酸制成盐酸盐,与丙炔腈在60℃反应1小时,即生成环胞苷盐酸盐,总收率68%。
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盐酸环胞苷文献

Cytosine-based nucleoside analogs are selectively lethal to DNA mismatch repair-deficient tumour cells by enhancing levels of intracellular oxidative stress.

Br. J. Cancer 108(4) , 983-92, (2013)

DNA mismatch repair deficiency is present in a significant proportion of a number of solid tumours and is associated with distinct clinical behaviour.To identify the therapeutic agents that might show...

Tyramine-like effect of cyclocytidine (2,2'-anhydro-1-β-arabinofuranosylcytosine hydrochloride), an antineoplastic agent Oguro, K., Hashimoto, K.

J. Exp. Med. 124 , 83-90, (1978)


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