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丙亚胺

丙亚胺用途

Razoxane(ICRF 159)是一种抗血管生成拓扑异构酶II抑制剂,可用于肾细胞癌(RCC)的研究[1]。

丙亚胺名称

[ CAS 号 ]:
21416-67-1

[ 中文名 ]:
丙亚胺

[ 英文名 ]:
Razoxane

[中文别名 ]:

[英文别名 ]:

4,4'-propylenebis(piperazine-2,6-dione)
4,4'-Propane-1,2-diyldipiperazine-2,6-dione
4,4'-(1-Methylethylene)bis(2,6-piperazinedione)
dl-1,2-bis(3,5-dioxopiperazin-1-yl)-propane
Propyliminum
RAZOXANUM
1,2-bis(3,5-dioxopiperazin-1-yl)-propane
(+)-1,2-bis(3,5-dioxopiperazinyl)propane
(+)-1,2-bis(3,5-dioxopiperazinyl-1-yl)propane
Razoxane

丙亚胺生物活性

[ 描述 ]:

Razoxane(ICRF 159)是一种抗血管生成拓扑异构酶II抑制剂,可用于肾细胞癌(RCC)的研究[1]。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶

[ 靶点 ]

Topoisomerase II

[体外研究]

在大鼠骨肉瘤模型中,Razoxane(30 mg/kg；i.p.)具有抗转移作用。

[体内研究]

早期使用Razoxane治疗(第2天至第14天,每天30毫克/千克)比后期治疗(移植后第14天至第28天,每天30毫克/千克,每天30毫克/千克)对肺转移的抑制作用更强【2】。动物模型：Sprague-Dawley大鼠【2】剂量：30毫克/千克或10毫克/千克/天给药：从肿瘤移植前2天到移植后14天腹腔内(i.p.)结果：导致中位生存时间的剂量依赖性延长(分别为83天或48天,而对照组为38天),但对原发肿瘤的生长没有影响。

[参考文献]

[1]. J P Braybrooke, et al. A phase II study of Razoxane, an antiangiogenic topoisomerase II inhibitor, in renal cell cancer with assessment of potential surrogate markers of angiogenesis. Clin Cancer Res.2000; 6(12):4697-704.

[2]. F Wingen, et al. Antimetastatic effects of Razoxane in a rat osteosarcoma model. Clin Exp Metastasis.Jan-Mar 1987; 5(1):9-16.

丙亚胺物理化学性质

[ 密度 ]:
1.333g/cm3

[ 沸点 ]:
531.5ºC at 760mmHg

[ 熔点 ]:
193ºC

[ 分子式 ]:
C₁₁H₁₆N₄O₄

[ 分子量 ]:
268.26900

[ 闪点 ]:
275.3ºC

[ 精确质量 ]:
268.11700

[ PSA ]:
98.82000

[ 蒸汽压 ]:
1.33E-13mmHg at 25°C

[ 折射率 ]:
1.534

[ 储存条件 ]:
room temp

[ 水溶解性 ]:
DMSO: soluble40mg/mL

丙亚胺MSDS

详细MSDS(安全技术说明书)

丙亚胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TL6389900

CHEMICAL NAME :: 2,6-Piperazinedione, 4,4'-propylenedi-

CAS REGISTRY NUMBER :: 21416-67-1

BEILSTEIN REFERENCE NO. :: 0821182

LAST UPDATED :: 199612

DATA ITEMS CITED :: 15

MOLECULAR FORMULA :: C11-H16-N4-O4

MOLECULAR WEIGHT :: 268.31

WISWESSER LINE NOTATION :: T6VMV ENTJ EY1&1- ET6VMV ENTJ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 3650 mg/kg/2Y-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - hematuria Blood - aplastic anemia

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 600 mg/kg/34W-I

TOXIC EFFECTS :: Blood - leukopenia

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 6467 mg/kg/6Y-I

TOXIC EFFECTS :: Blood - normocytic anemia Blood - thrombocytopenia

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 500 mg/kg

TOXIC EFFECTS :: Tumorigenic - active as anti-cancer agent

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 693 mg/kg/77W-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Blood - leukemia

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 4650 mg/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Blood - leukemia

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 2693 mg/kg/3Y-C

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Skin and Appendages - tumors

TYPE OF TEST :: TD - Toxic dose (other than lowest)

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 3650 mg/kg/2Y-I

TOXIC EFFECTS :: Tumorigenic - Carcinogenic by RTECS criteria Blood - leukemia

TYPE OF TEST :: Micronucleus test

MUTATION DATA

TEST SYSTEM :: Rodent - hamster

DOSE/DURATION :: 100 mg/kg

REFERENCE :: BJCAAI British Journal of Cancer. (Macmillan Press Ltd., Houndmills, Basingstoke, Hants. RG21 2XS, UK) V.1- 1947- Volume(issue)/page/year: 52,725,1985

丙亚胺安全信息

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

[ RTECS号 ]:
TL6389900

丙亚胺文献

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

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J. Clin. Oncol. 30(10) , 1042-9, (2012)

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丙亚胺