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比卡鲁胺

比卡鲁胺用途

Bicalutamide是非甾体雄激素受体抑制剂。

比卡鲁胺名称

[ CAS 号 ]:
90357-06-5

[ 中文名 ]:
比卡鲁胺

[ 英文名 ]:
Bicalutamide

[中文别名 ]:

[英文别名 ]:

Bicaiutamide
25mg
ODEX
BicalutaMide API
MFCD00869971
R-bicalutamide
Bicalutamide
R-Bicalutimide
Cosudex

比卡鲁胺生物活性

[ 描述 ]:

Bicalutamide是非甾体雄激素受体抑制剂。

[ 相关类别 ]:

信号通路 >> 其他 >> 雄激素受体

信号通路 >> 自噬 >> 自噬

研究领域 >> 癌症

[参考文献]

[1]. Nicola J. Clegg,1 John Wongvipat,1,2 Jim Joseph, ARN-509: a novel anti-androgen for prostate cancer treatment. Cancer Res. 2012 March 15; 72(6): 1494-1503.

[2]. RACHEL M. SQUILLACE, DAVID MILLER, SCOTT D. WARDWELL, Synergistic activity of the mTOR inhibitor ridaforolimus and the antiandrogen bicalutamide in prostate cancer models. Int J Oncol. 2012 August; 41(2): 425-432.

[3]. Nakabayashi M, Werner L, Courtney KD, Phase II trial of RAD001 and bicalutamide for castration-resistant prostate cancer. BJU Int. 2012 Dec;110(11):1729-35.

[相关活性小分子]

比卡鲁胺物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
650.3±55.0 °C at 760 mmHg

[ 熔点 ]:
191-193°C

[ 分子式 ]:
C₁₈H₁₄F₄N₂O₄S

[ 分子量 ]:
430.373

[ 闪点 ]:
347.1±31.5 °C

[ 精确质量 ]:
430.061035

[ PSA ]:
115.64000

[ LogP ]:
4.94

[ 外观性状 ]:
灰白色结晶固体

[ 蒸汽压 ]:
0.0±2.0 mmHg at 25°C

[ 折射率 ]:
1.578

[ 储存条件 ]:
Store at RT

比卡鲁胺MSDS

比卡鲁胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TX1413500

CHEMICAL NAME :: Propanamide, N-(4-cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophe nyl)sulfonyl)-2-hydro xy-2- methyl-, (+-)-

CAS REGISTRY NUMBER :: 90357-06-5

LAST UPDATED :: 199712

DATA ITEMS CITED :: 5

MOLECULAR FORMULA :: C18-H14-F4-N2-O4-S

MOLECULAR WEIGHT :: 430.40

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/kg

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

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 22,75,1997

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

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

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 22,75,1997

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >2 gm/kg

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

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 22,75,1997 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 420 mg/kg

SEX/DURATION :: female 21 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - other effects on male Endocrine - changes in luteinizing hormone

REFERENCE :: ACENA7 Acta Endocrinologica (Copenhagen). (Periodica, Skolegade 12 E, DK-2500 Valby, Denmark) V.1- 1948- Volume(issue)/page/year: 125,547,1991

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 420 mg/kg

SEX/DURATION :: female 21 day(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - spermatogenesis (incl. genetic material, sperm morphology, motility, and count) Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands

REFERENCE :: ACENA7 Acta Endocrinologica (Copenhagen). (Periodica, Skolegade 12 E, DK-2500 Valby, Denmark) V.1- 1948- Volume(issue)/page/year: 125,547,1991

比卡鲁胺安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

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

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
3077

[ RTECS号 ]:
TX1413500

[ 包装等级 ]:
III

[ 危险类别 ]:
9

[ 海关编码 ]:
2929909090

比卡鲁胺合成路线

比卡鲁胺上下游产品

比卡鲁胺上游产品

比卡鲁胺下游产品

比卡鲁胺制备

2-甲基丙烯酸甲酯(I)环氧化得到环氧化物(Ⅱ)，再和对氟苯硫酚在氢化钠作用下反应，生成化合物(Ⅲ)，接着氧化为化合物(Ⅳ)。然后水解为酸(V)，用氯化亚砜氯化为酰氯(VI)。最后和3-三氟甲基-4-氰基苯胺(Ⅶ)缩合，得到产物。

比卡鲁胺海关

[ 海关编码 ]: 2929909090

[ 中文概述 ]:
2929909090 其他含氮基化合物. 增值税率:17.0% 退税率:9.0% 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

[ Summary ]:
2929909090 other compounds with other nitrogen function VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%

比卡鲁胺文献

CYP3A5 regulates prostate cancer cell growth by facilitating nuclear translocation of AR.

Prostate 75(5) , 527-38, (2015)

The central role of androgen receptor (AR) signaling is established in prostate cancer growth and progression. We propose CYP3A5 is part of a feedback loop that modulates the sensitivity of AR to andr...

Differential androgen deprivation therapies with anti-androgens casodex/bicalutamide or MDV3100/Enzalutamide versus anti-androgen receptor ASC-J9(R) Lead to promotion versus suppression of prostate cancer metastasis.

J. Biol. Chem. 288(27) , 19359-69, (2013)

Despite the fact that androgen deprivation therapy (ADT) can effectively reduce prostate cancer (PCa) size, its effect on PCa metastasis remains unclear. We examined the existing data on PCa patients ...

TLR3 engagement induces IRF-3-dependent apoptosis in androgen-sensitive prostate cancer cells and inhibits tumour growth in vivo.

J. Cell. Mol. Med. 19(2) , 327-39, (2015)

Toll-like receptors (TLRs) are a family of highly conserved transmembrane proteins expressed in epithelial and immune cells that recognize pathogen associated molecular patterns. Besides their role in...

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