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氟达拉滨

氟达拉滨用途

【用途一】
其磷酸基在血液中被迅速裂开，余下的2-氟阿糖腺苷(Fara-A)则进入细胞内，并被磷酸化成为具有活性的代谢物Farar-ATP而发挥作用。用于慢性淋巴细胞白血症。

氟达拉滨名称

[ CAS 号 ]:
21679-14-1

[ 中文名 ]:
氟达拉宾

[ 英文名 ]:
Fludarabine

[中文别名 ]:

[英文别名 ]:

UNII-P2K93U8740
9-b-D-Arabinofuranosyl-2-fluoro-9H-purin-6-amine
9-β-D-Arabinofuranosyl-2-fluoroadenine
MFCD00132942
9H-Purin-6-amine, 9-β-D-arabinofuranosyl-2-fluoro-
Fludarabine des-phosphate
9-(β-D-Arabinofuranosyl)-2-fluoro-9H-purin-6-amine
9-b-D-Arabinofuranosyl-2-fluoroadenine
Fludarabine
EINECS 244-525-5

氟达拉滨生物活性

[ 描述 ]:

Fludarabine(NSC 118218)是DNA合成抑制剂。

[ 相关类别 ]:

信号通路 >> 细胞周期/DNA损伤 >> 核苷抗代谢药/类似物

研究领域 >> 癌症

[参考文献]

[1]. Rai KR, et al. Fludarabine compared with chlorambucil as primary therapy for chronic lymphocytic leukemia. N Engl J Med. 2000 Dec 14;343(24):1750-7.

[2]. Tournilhac O, et al. Impact of frontline fludarabine and cyclophosphamide combined treatment on peripheral blood stem cell mobilization in B-cell chronic lymphocytic leukemia. Blood. 2004 Jan 1;103(1):363-5. Epub 2003 Sep 11.

[相关活性小分子]

氟达拉滨物理化学性质

[ 密度 ]:
2.2±0.1 g/cm3

[ 沸点 ]:
747.3±70.0 °C at 760 mmHg

[ 熔点 ]:
265-268ºC

[ 分子式 ]:
C₁₀H₁₂FN₅O₄

[ 分子量 ]:
285.232

[ 闪点 ]:
405.8±35.7 °C

[ 精确质量 ]:
285.087341

[ PSA ]:
139.54000

[ LogP ]:
-0.40

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
0.0±2.6 mmHg at 25°C

[ 折射率 ]:
1.876

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
DMF: 20 mg/mL, clear, faintly yellow

氟达拉滨MSDS

详细MSDS(安全技术说明书)

氟达拉滨毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AU6207000

CHEMICAL NAME :: Adenine, 9-beta-D-arabinofuranosyl-2-fluoro-

CAS REGISTRY NUMBER :: 21679-14-1

LAST UPDATED :: 198909

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C10-H12-F-N5-O4

MOLECULAR WEIGHT :: 285.27

WISWESSER LINE NOTATION :: T56 BN DN FN HNJ GF IZ D- BT5OTJ CQ DQ E1Q

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 375 mg/kg

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: DNA inhibition

MUTATION DATA

TYPE OF TEST :: Mutation in mammalian somatic cells

TEST SYSTEM :: Rodent - hamster Ovary

DOSE/DURATION :: 100 umol/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 210,291,1989

氟达拉滨安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R23/24/25;R36/37/38;R39

[ 安全声明 (欧洲) ]:
S26-S36/37-S45

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

[ WGK德国 ]:
3

[ RTECS号 ]:
AU6207000

氟达拉滨制备

【方法一】
2，4，5，6-四氨基嘧啶和甲酰胺一起加热环合，得2，6-二氨基嘌呤。用乙酸酐-吡啶络合物酰化，得2，6-二乙酰胺基嘌呤。接着和2，3，5-三-O-苄基-D阿拉伯呋喃糖基氯化物反应，得化合物(I)。(I)脱乙酰化得化合物(Ⅱ)。(II)在氟硼酸-四氢呋喃中，先亚硝化，再取代，得化合物(IlI)。在三氯化硼作用下，脱去苄基得氟达拉滨。以2，3，5-三-O-苄基-D-阿拉伯呋喃糖基氯化物计，收率17.5%。

氟达拉滨文献

Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).

J. Sci. Ind. Res. 65(10) , 808, (2006)

Drug-induced liver injury (DILI) is a significant concern in drug development due to the poor concordance between preclinical and clinical findings of liver toxicity. We hypothesized that the DILI typ...

Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.

J. Med. Chem. 51 , 6740-51, (2008)

The work provides a new model for the prediction of the MAO-A and -B inhibitor activity by the use of combined complex networks and QSAR methodologies. On the basis of the obtained model, we prepared ...

Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.

Drug Metab. Dispos. 36 , 1385-405, (2008)

We present herein a compilation and trend analysis of human i.v. pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic ...

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