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羟基氟他胺

羟基氟他胺用途

羟氟他胺(HF)是氟他胺的活性代谢物,是一种有效的雄激素受体拮抗剂(IC50=700nm)。羟基氟他胺可用于前列腺癌的研究[1][2]。

羟基氟他胺名称

[ CAS 号 ]:
52806-53-8

[ 中文名 ]:
羟基氟他胺

[ 英文名 ]:
2-Hydroxyflutamide

[中文别名 ]:

[英文别名 ]:

2-hydroxy Flutamide
Hydroxyflutamide
2-Hydroxy-flutamide

羟基氟他胺生物活性

[ 描述 ]:

羟氟他胺(HF)是氟他胺的活性代谢物,是一种有效的雄激素受体拮抗剂(IC50=700nm)。羟基氟他胺可用于前列腺癌的研究[1][2]。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 其他 >> 雄激素受体

[ 靶点 ]

IC50: 700 nM (androgen receptor)[1]

[参考文献]

[1]. Furr BJ, et, al. Casodex: preclinical studies and controversies. Ann N Y Acad Sci. 1995 Jun 12;761:79-96.

[2]. Liu HL, et, al. A Molecular Modeling Study of the Hydroxyflutamide Resistance Mechanism Induced by Androgen Receptor Mutations. Int J Mol Sci. 2017 Aug 23;18(9):1823.

羟基氟他胺物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
443.8±45.0 °C at 760 mmHg

[ 熔点 ]:
125-130â„ƒ

[ 分子式 ]:
C₁₁H₁₁F₃N₂O₄

[ 分子量 ]:
292.211

[ 闪点 ]:
222.2±28.7 °C

[ 精确质量 ]:
292.067078

[ PSA ]:
95.15000

[ LogP ]:
3.16

[ 外观性状 ]:
固体;White to Brown powder to crystal

[ 蒸汽压 ]:
0.0±1.1 mmHg at 25°C

[ 折射率 ]:
1.546

[ 储存条件 ]:
室温，干燥

羟基氟他胺MSDS

详细MSDS(安全技术说明书)

羟基氟他胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TX1466250

CHEMICAL NAME :: Propanamide, 2-hydroxy-2-methyl-N-(4-nitro-3-(trifluoromethyl)phen yl)-

CAS REGISTRY NUMBER :: 52806-53-8

LAST UPDATED :: 199706

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C11-H11-F3-O2-N4

MOLECULAR WEIGHT :: 288.26

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 60 mg/kg/6D-I

TOXIC EFFECTS :: Endocrine - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - dehydrogenases

REFERENCE :: JJATDK JAT, Journal of Applied Toxicology. (John Wiley & Sons Ltd., Baffins Lane, Chichester, W. Sussex PO19 1UD, UK) V.1- 1981- Volume(issue)/page/year: 1,297,1981 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 6 gm/kg

SEX/DURATION :: female 11-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - other effects on male

REFERENCE :: CJPPA3 Canadian Journal of Physiology and Pharmacology. (National Research Council of Canada, Publication Sales and Distribution, Ottawa ON K1A OR6, Canada) V.42- 1964- Volume(issue)/page/year: 73,1582,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2400 mg/kg

SEX/DURATION :: female 15-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands Reproductive - Paternal Effects - other effects on male

REFERENCE :: CJPPA3 Canadian Journal of Physiology and Pharmacology. (National Research Council of Canada, Publication Sales and Distribution, Ottawa ON K1A OR6, Canada) V.42- 1964- Volume(issue)/page/year: 73,1582,1995

羟基氟他胺安全信息

[ 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

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

[ RTECS号 ]:
TX1466250

[ 海关编码 ]:
2924299090

羟基氟他胺上下游产品

羟基氟他胺上游产品

羟基氟他胺下游产品

羟基氟他胺海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

羟基氟他胺文献

Metabolism of UV-filter benzophenone-3 by rat and human liver microsomes and its effect on endocrine-disrupting activity.

Toxicol. Appl. Pharmacol. 282(2) , 119-28, (2015)

Benzophenone-3 (2-hydroxy-4-methoxybenzophenone; BP-3) is widely used as sunscreen for protection of human skin and hair from damage by ultraviolet (UV) radiation. In this study, we examined the metab...

GATA3 in the urinary bladder: suppression of neoplastic transformation and down-regulation by androgens.

Am. J. Cancer Res. 4(5) , 461-73, (2014)

Recent evidence suggests the involvement of sex hormone receptors in bladder cancer initiation, while precise functions of androgens and estrogens in the carcinogenesis step remain poorly understood. ...

TRPM8 channel as a novel molecular target in androgen-regulated prostate cancer cells.

Oncotarget 6 , 17221-36, (2015)

The cold and menthol receptor TRPM8 is highly expressed in prostate and prostate cancer (PC). Recently, we identified that TRPM8 is as an ionotropic testosterone receptor. The TRPM8 mRNA is expressed ...

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