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氟西他宾

氟西他宾用途

氟罗西他滨是阿糖胞苷的一种含氟酰肼类似物,在体内部分水解成两种活性抗肿瘤物质(阿糖基三氟胞苷(ara-FC)和阿糖基氟尿嘧啶(ara-FU))。氟罗西他滨在急性白血病和实体瘤的I期研究中具有抗肿瘤活性[1]。

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氟西他宾名称

[ CAS 号 ]:
37717-21-8

[ 中文名 ]:
氟西他宾

[ 英文名 ]:
Flurocitabine

[中文别名 ]:

[英文别名 ]:

5-fluoro-arabino-O2,O2'-cyclocytidine
Ro-21-0702
fluoroancitabine
5-Fluoro-2,2'-cyclocytidine
5-fluoro-arabino-2,2'-anhydro-cytidine
Fluorocitabin
5-Fluor-2,2'-cyclocytidin
AAFC

氟西他宾生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> 核苷抗代谢药/类似物

[参考文献]

[1]. Alberto P, et al. Phase II study of anhydro-ara-5-fluorocytidine in adenocarcinoma of gastrointestinal tract, epidermoid carcinoma of lung, head and neck, breast carcinoma and small cell anaplastic carcinoma of lung. A study report of the E.O.R.T.C. early clinical trial cooperative group. Eur J Cancer. 1978;14(2):195-201.

氟西他宾物理化学性质

[ 密度 ]:
2.11g/cm3

[ 沸点 ]:
391.7ºC at 760mmHg

[ 分子式 ]:
C₉H₁₀FN₃O₄

[ 分子量 ]:
243.19200

[ 闪点 ]:
190.7ºC

[ 精确质量 ]:
243.06600

[ PSA ]:
100.59000

[ 折射率 ]:
1.813

氟西他宾毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HA5400000

CHEMICAL NAME :: Cytosine, 2,2'-anhydroarabino-5-fluoro-

CAS REGISTRY NUMBER :: 37717-21-8

LAST UPDATED :: 199706

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C9-H10-F-N3-O4

MOLECULAR WEIGHT :: 243.22

WISWESSER LINE NOTATION :: T B556 AN CO GO IN HHTT&J D1Q EQ JZ KF

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Human

DOSE/DURATION :: 33 mg/kg

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting Blood - normocytic anemia Blood - leukopenia

MUTATION DATA

TYPE OF TEST :: DNA inhibition

TEST SYSTEM :: Rodent - mouse Leukocyte

DOSE/DURATION :: 1 mmol/L

REFERENCE :: BCPCA6 Biochemical Pharmacology. (Pergamon Press Inc., Maxwell House, Fairview Park, Elmsford, NY 10523) V.1- 1958- Volume(issue)/page/year: 23,2657,1974