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82413-20-5生产厂家

82413-20-5价格

82413-20-5

82413-20-5结构式
82413-20-5结构式
  • 常用中文名:屈洛昔芬
  • 常用英文名:Droloxifene
  • CAS号:82413-20-5
  • 分子式:C26H29NO2
  • 分子量:579.63700
  • 相关类别: 原料药 抗肿瘤药 激素类抗肿瘤药
  • 发布时间:2018-09-17 11:56:08
  • 更新时间:2024-01-02 19:36:58
  • Droloxifene,Tamoxifen 衍生物,是一种具有口服活性和选择性的雌激素受体 (estrogen receptor) 调节剂。Droloxifene 具有抗雌激素和抗植入作用。Droloxifene 诱导 MCF-7 细胞 p53 表达及凋亡。Droloxifene 预防去卵巢大鼠骨丢失。

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中文名 屈洛昔芬
英文名 3-[(E)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol
中文别名 3-[1-[4-(2-二甲基氨基乙氧基)苯基]-2-苯基丁-1-烯基]苯酚
屈洛昔酚
英文别名 (E)-1-(4'-(2-dimethylaminoethoxy)phenyl)-1-(3-hydroxyphenyl)-2-phenylbut-1-ene
Droloxifenum [Latin]
Droloxifene
K 060
K 060E
MFCD00468089
FK-435
E-1-[4'-(2-dimethylaminoethoxy)-phenyl]-1-(3'-hydroxyphenyl)-2-phenyl-1-butene
E-Droloxifene
Droloxifeno [Spanish]
3-Hydroxytamoxifen
描述 Droloxifene,Tamoxifen 衍生物,是一种具有口服活性和选择性的雌激素受体 (estrogen receptor) 调节剂。Droloxifene 具有抗雌激素和抗植入作用。Droloxifene 诱导 MCF-7 细胞 p53 表达及凋亡。Droloxifene 预防去卵巢大鼠骨丢失。
相关类别
体外研究 Droloxifene(10nm;16-18h)诱导MCF-7细胞凋亡[1]。细胞活力测定[2]细胞株:MCF-7细胞浓度:10nm培养时间:16-18h结果:诱导细胞凋亡
体内研究 屈洛昔芬(5-20 mg/kg;p.o.;每日4周)以10 mg/kg的剂量增加DFM的骨密度,并完全防止20 mg/kg/天的剂量降低去卵巢(OVX)引起的DFM的骨密度和骨密度[3]。动物模型:5月龄假手术大鼠[3]剂量:5、10、20 mg/kg口服;每日4周结果:10 mg/kg时DFM的骨密度显著增加;20 mg/kg/d时完全阻止OVX所致DFM的骨密度和骨密度下降。
参考文献

[1]. Herrington DM, et al. Cardiovascular effects of droloxifene, a new selective estrogen receptor modulator, in healthypostmenopausal women. Arterioscler Thromb Vasc Biol. 2000 Jun;20(6):1606-12.

[2]. Grasser WA, et al. Common mechanism for the estrogen agonist and antagonist activities of droloxifene. J Cell Biochem. 1997 May;65(2):159-71.

[3]. Ke HZ, et al. Droloxifene, a new estrogen antagonist/agonist, prevents bone loss in ovariectomized rats. ndocrinology. 1995 Jun;136(6):2435-41.

[4]. Huang Y, et al. Anti-implantation effect of droloxifene in rats and its relationship with anti-estrogenic activity. Acta Pharmacol Sin. 2005 Oct;26(10):1243-7.

密度 1.092 g/cm3
沸点 526.6ºC at 760 mmHg
熔点 127-129ºC
分子式 C26H29NO2
分子量 579.63700
精确质量 579.24700
PSA 164.83000
LogP 4.45320
外观性状 灰白色至灰白的-米色固体
折射率 1.596
储存条件 Amber Vial, -20°C Freezer

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SL1209900
CHEMICAL NAME :
Phenol, 3-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-2-phenyl-1-b utenyl)-, (E)-
CAS REGISTRY NUMBER :
82413-20-5
LAST UPDATED :
199704
DATA ITEMS CITED :
7
MOLECULAR FORMULA :
C26-H29-N-O2
MOLECULAR WEIGHT :
387.56

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>4500 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 9,186,1984
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>2250 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 9,186,1984
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>3 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 9,186,1984
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
>1500 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 9,186,1984 *** REVIEWS *** IARC Cancer Review:Human Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 66,241,1996 IARC Cancer Review:Animal Inadequate Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 66,241,1996 IARC Cancer Review:Group 3 IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 66,241,1996

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