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替拉扎明

替拉扎明用途

Tirapazamine是一种抗癌剂,对实体瘤中的缺氧细胞具有选择性细胞毒性,从而诱导DNA中的单链和双链断裂,碱基损伤和细胞死亡。

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替拉扎明名称

[ CAS 号 ]:
27314-97-2

[ 中文名 ]:
替拉扎明

[ 英文名 ]:
Tirapazamine

[中文别名 ]:

[英文别名 ]:

4-hydroxy-1-oxido-1,2,4-benzotriazin-1-ium-3-imine
1,2,4-Benzotriazin-3-amine, 1,4-dioxide
3-Amino-1,2,4-benzotriazine 1,4-Dioxide
1,4-Dioxido-1,2,4-benzotriazin-3-ylamine
SR 259075
1,2,4-Benzotriazin-3-amine 1,4-dioxide
Tirazone
Tirapazamine
3-Aminobenzo[e][1,2,4]triazine 1,4-dioxide

替拉扎明生物活性

[ 描述 ]:

Tirapazamine是一种抗癌剂,对实体瘤中的缺氧细胞具有选择性细胞毒性,从而诱导DNA中的单链和双链断裂,碱基损伤和细胞死亡。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 癌症

[参考文献]

[1]. Cai TY, et al. Tirapazamine sensitizes hepatocellular carcinoma cells to topoisomerase I inhibitors via cooperative modulation of hypoxia-inducible factor-1α. Mol Cancer Ther. 2014 Mar;13(3):630-42.

[2]. Sliwinska J, et al. Tirapazamine-doxorubicin interaction referring to heart oxidative stress and Ca2? balance protein levels. Oxid Med Cell Longev. 2012;2012:890826.

[相关活性小分子]

替拉扎明物理化学性质

[ 密度 ]:
1.7±0.1 g/cm3

[ 沸点 ]:
493.6±28.0 °C at 760 mmHg

[ 熔点 ]:
220ºC

[ 分子式 ]:
C₇H₆N₄O₂

[ 分子量 ]:
178.148

[ 闪点 ]:
252.3±24.0 °C

[ 精确质量 ]:
178.049072

[ PSA ]:
89.83000

[ LogP ]:
-0.31

[ 外观性状 ]:
橙色-红色结晶粉末

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.777

[ 储存条件 ]:
0-10°C;避免加热

替拉扎明毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DM0671500

CHEMICAL NAME :: 1,2,4-Benzotriazine, 3-amino-, 1,4-dioxide

CAS REGISTRY NUMBER :: 27314-97-2

BEILSTEIN REFERENCE NO. :: 0179322

LAST UPDATED :: 199712

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C7-H6-N4-O2

MOLECULAR WEIGHT :: 178.17

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 59390 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >36 mg/kg

TOXIC EFFECTS :: Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Endocrine - other changes Blood - changes in bone marrow (not otherwise specified)

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 89 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 :: 101 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Skin and Appendages - hair Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 19 mg/kg/2W-C

TOXIC EFFECTS :: Related to Chronic Data - death

MUTATION DATA

TYPE OF TEST :: Unscheduled DNA synthesis

TEST SYSTEM :: Rodent - rat Mammary gland

DOSE/DURATION :: 500 umol/L

REFERENCE :: CRNGDP Carcinogenesis (London). (Oxford Univ. Press, Pinkhill House, Southfield Road, Eynsham, Oxford OX8 1JJ, UK) V.1- 1980- Volume(issue)/page/year: 11,1407,1990

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替拉扎明安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
26-36

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

[ RTECS号 ]:
DM0671500

替拉扎明合成路线

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替拉扎明文献

An innovative three-dimensional gelatin foam culture system for improved study of glioblastoma stem cell behavior.

J. Biomed. Mater. Res. B. Appl. Biomater. 103(3) , 618-28, (2015)

Three-dimensional (3-D) tissue engineered constructs provide a platform for examining how the local extracellular matrix contributes to the malignancy of various cancers, including human glioblastoma ...

Tirapazamine-doxorubicin interaction referring to heart oxidative stress and Ca²⁺ balance protein levels.

Oxid. Med. Cell. Longev. 2012 , 890826, (2012)

Doxorubicin (DOX) causes long-term cardiomyopathy that is dependent on oxidative stress and contractility disorders. Tirapazamine (TP), an experimental adjuvant drug, passes the same red-ox transforma...

Exploiting tumour hypoxia and overcoming mutant p53 with tirapazamine.

Br. J. Cancer 77 Suppl 4 , 12-4, (1998)

Human solid tumours are composed of a significant proportion of hypoxic cells, i.e. cells with oxygen levels lower than those of normal tissues. Tumour hypoxic cells have been shown to have a negative...

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