CAS 90357-06-5; 比卡鲁胺; propanamide, n-(4-cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)

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货号

品牌

产品名称

规格

包装、参考价格

详情

B797270

MACKLIN

毕卡鲁胺

10mM in DMSO

562元/1ml;

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储存：-20°C

B803285

MACKLIN

毕卡鲁胺

≥98% (HPLC), powder

27元/10mg; 40元/50mg; 49元/200mg; 101元/1g; 340元/5g; 1300元/25g;

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储存：室温
状态：粉末

B3206

TCI

Bicalutamide

>98.0%(HPLC)(N)

100元/200MG; 290元/1G;

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基本信息

纯度/分析方法	>98.0%(HPLC)(N)
分子式/分子量	C₁₈H₁₄F₄N₂O₄S = 430.37
外观与形状(20℃)	固体
Reaxys-RN	5364666
PubChem物质ID	172088993
Merck Index (14)	1200
MDL编号	MFCD00869971

技术规格

Appearance	White to Almost white powder to crystal
Purity(HPLC)	min. 98.0 area%
Purity(with Total Nitrogen)	min. 98.0 %
Melting point	194.0 to 198.0 ℃

物性(参考值)

熔点	196 ℃
最大吸收波长	270(CH3CN) nm

安全信息

图形或危害标志
信号词	危险
危险性说明	H315 : 造成皮肤刺激。 H319 : 造成严重眼刺激。 H360 : 可能对生育能力或胎儿造成伤害。
防范说明	P501 : 将内装物/容器送到批准的废物处理厂处理。 P202 : 在阅读并明了所有安全措施前切勿搬动。 P201 : 使用前取得专用说明。 P264 : 作业后彻底清洗皮肤。 P280 : 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302 + P352 : 如皮肤沾染：用水充分清洗。 P308 + P313 : 如接触到或有疑虑：求医/就诊。 P337 + P313 : 如仍觉眼刺激：求医/就诊。 P305 + P351 + P338 : 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P362+P364 : 脱掉沾污的衣服，清洗后方可重新使用。 P332 + P313 : 如发生皮肤刺激：求医/就诊。 P405 : 存放处须加锁。

相关法规

RTECS#

TX1413500

956180

J&K

Bicalutamide

99%, 一种非甾体雄激素受体抑制剂

314元/200MG; 962元/1G;

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基本信息

分子式	C₁₈H₁₄F₄N₂O₄S
分子量	430.37
沸点	194-198
MDL编码	MFCD00869971
Merck	14,1200
存储条件	Freezer -20℃

产品描述

Bicalutamide是一种androgen receptor (AR)拮抗剂，在LNCaP/AR(cs)细胞系中IC50为0.16 μM。

靶点（IC50 & Targe）

Androgen Receptor,0.16μM

体外研究

Bicalutamide 经过一个拮抗剂到激活剂的转变，刺激AR活性。在缺乏合成雄激素R1881的情况下，Bicalutamide处理LNCaP/AR(cs)细胞，改变基因表达，与其记录的良好激活剂活性相符合。Bicalutamide诱导细胞增殖，这种作用存在剂量依赖性，且只部分抗R1881的效果。Bicalutamide 处理呀显著产生大量核AR,虽然比R1881处理的少。Bicalutamide通过诱导DNA在AR靶基因结合，而具有部分激活剂活性，且不完全抗 R1881的效果。在R1881存在时, Bicalutamide部分激活 VP16-AR调节的转录，指导AR 结合到DNA上。使用AR驱动的荧光素酶报告结构稳定整合到LNCaP/AR-luc细胞中。在R1881存在时, Bicalutamide只微弱且部分抗 VP16-AR调节的转录，IC50 为 0.35 μM。[1] 微摩尔 Bicalutamide显著降低集落形成，这种作用存在剂量依赖性。[2] 双重抑制 AR 和 mTOR信号通路产生进一步好处，在体外，Ridaforolimus-Bicalutamide联用作用于前列腺癌细胞，与单独药剂处理相比，产生协同抗增殖效果。[3]

体内研究

Bicalutamide按规定的次最大剂量单独处理，降低79%肿瘤生长。Ridaforolimus-Bicalutamide 联用具有改进的和有效的抗肿瘤活性，几乎完全废除肿瘤生长。联合使用具有良好耐受性，在处理过程中体重没有明显改变。联用处理的小鼠中，血浆PSA水平与肿瘤生长紧密相关。[3]

激酶实验

Whole-cell competitive binding assays:

Whole-cell competitive binding assays are performed in LNCaP/AR(codon-switch) (LNCaP/AR(cs)) (harbors a mixture of exogenous wild-type AR and endogenous mutant AR (T877A)) and cells propagated in Iscove's or RPMI media supplemented with 10% fetal bovine serum, or during the assay with 10% charcoal-stripped, dextran-treated fetal bovine serum (CSS). Cells are pre-incubated with 18F-FDHT, increasing concentrations (1pM to 1μM) of cold Bicalutamide are added, and the assay is performed to measure specific uptake of 18F-FDHT (4). IC50 values are determined using a one site binding model with least squares curve fitting and R2 > 0.99.

细胞实验

Cell lines: C4-2细胞系

Concentrations: 0 nM-1 μM

Incubation Time: 72小时

Method: 指数生长的C4-2细胞接种到96孔板中，在37oC下温育过夜。24小时后，吸除其中一个板，然后储存在-80oC中，其他使用10倍系列浓度 Ridaforolimus(1000 nM 到0.0001 nM)或乙醇（对照）处理。在 37oC下培养72小时，使用Cy qUANT细胞增殖检测试剂盒测评细胞生长。

(Only for Reference)

动物实验

Animal Models: 携带C4-2细胞的雄性裸鼠

Formulation: 4% 乙醇, 5% Tween-80, 和 5% PEG

Dosages: 10 mg/kg

Administration: 口服处理

(Only for Reference)

参考文献

[1] Clegg NJ, et al. Cancer Res. 2012, 72(6), 1494-1503.

[2] Colquhoun AJ, et al. Prostate Cancer Prostatic Dis. 2012.

[3] Squillace RM, et al. Int J Oncol. 2012.

安全信息

防范说明	P262
RTECS	TX1413500

C46100

Alfa Aesar

Bicalutamide

97%

5055元/1g;

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基本信息

Ref#
46100

分子式
C18H14F4N2O4S

GHS危害和防范说明

Hazard Statements
H315 H319 H335 H360

Precautionary Statements
P302+P352 P337+P313 P304+P340 P312 P280 P332+P313

PHR1678

Supelco

Bicalutamide

Pharmaceutical Secondary Standard; Certified Reference Material

976.29元/1 G;

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产品说明

一般描述

Pharmaceutical secondary standards for application in quality control, provide pharma laboratories and manufacturers with a convenient and cost-effective alternative to the preparation of in-house working standards. Bicalutamide is a non-steroidal peripheral androgen receptor inhibitor. Its mode of action involves inhibiting androgen by binding to cytosol androgen receptors in the target tissue.

应用

These Secondary Standards are qualified as Certified Reference Materials. These are suitable for use in several analytical applications including but not limited to pharma release testing, pharma method development for qualitative and quantitative analyses, food and beverage quality control testing, and other calibration requirements.
Bicalutamide may be used as a pharmaceutical reference standard for the determination of the analyte by high performance liquid chromatography and UV spectrophotometry.

生化/生理作用

比卡鲁胺 (CDX) 是一种非杀菌的雄激素受体 (AR) 拮抗剂，是纯抗雄激素。它通过平衡组蛋白乙酰化/去乙酰化和共调剂募集发挥作用。比卡鲁胺(CDX)消除了雄激素介导的表达。例如，前列腺癌、PLZF(早幼粒细胞白血病锌指蛋白)和GADD45γ中的MMP13上调(生长停滞和可诱导的DNA损伤，γ)。通过雄激素，对PI3K /AKT磷酸化进行非基因组、非转录依赖性刺激，抑制比卡鲁胺(CDX)。

分析说明

These secondary standards offer multi-traceability to the USP, EP and BP primary standards, where they are available.

其他说明

This Certified Reference Material (CRM) is produced and certified in accordance with ISO 17034 and ISO/IEC 17025. All information regarding the use of this CRM can be found on the certificate of analysis.

附注

To see an example of a Certificate of Analysis for this material enter LRAA6123 in the slot below. This is an example certificate only and may not be the lot that you receive.

基本信息

经验(实验)分子式	C₁₈H₁₄F₄N₂O₄S
分子量	430.37
MDL编号	MFCD00869971
PubChem化学物质编号	329823550
NACRES	NA.24

产品性质

质量水平	300
等级	certified reference material pharmaceutical secondary standard
CofA	current certificate can be downloaded
包装	pkg of 1 g
technique(s)	HPLC: suitable gas chromatography (GC): suitable
application(s)	pharmaceutical (small molecule)
格式	neat
药典可追溯性	traceable to BP 1115 traceable to PhEur Y0001444 traceable to USP 1071202
储存温度	2-8℃
SMILES string	CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc2ccc(C#N)c(c2)C(F)(F)F
InChI	1S/C18H14F4N2O4S/c1-17(26,10-29(27,28)14-6-3-12(19)4-7-14)16(25)24-13-5-2-11(9-23)15(8-13)18(20,21)22/h2-8,26H,10H2,1H3,(H,24,25)
InChI key	LKJPYSCBVHEWIU-UHFFFAOYSA-N
Gene Information	human ... AR(367)

安全信息

象形图
警示用语：	Danger
危险声明	H351 - H360FD - H410
预防措施声明	P202 - P273 - P280 - P308 + P313 - P391 - P405
危险分类	Aquatic Chronic 1 - Carc. 2 - Repr. 1B
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

Y0001444

Bicalutamide

European Pharmacopoeia (EP) Reference Standard

1277.32元/ ;

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产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.For further information and support please go to the website of the issuing Pharmacopoeia.

生化/生理作用

包装

Unit quantity: 160 mg. Subject to change. The product is delivered as supplied by the issuing Pharmacopoeia. For the current unit quantity, please visit the EDQM reference substance catalogue.

注意

Please find SDS provided by EDQM here..

其他说明

Sales restrictions may apply.

基本信息

经验(实验)分子式	C₁₈H₁₄F₄N₂O₄S
分子量	430.37
MDL编号	MFCD00869971
PubChem化学物质编号	329831426
NACRES	NA.24

产品性质

等级	pharmaceutical primary standard
manufacturer/tradename	EDQM
application(s)	pharmaceutical (small molecule)
格式	neat
储存温度	2-8℃
SMILES string	CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc2ccc(C#N)c(c2)C(F)(F)F
InChI	1S/C18H14F4N2O4S/c1-17(26,10-29(27,28)14-6-3-12(19)4-7-14)16(25)24-13-5-2-11(9-23)15(8-13)18(20,21)22/h2-8,26H,10H2,1H3,(H,24,25)
InChI key	LKJPYSCBVHEWIU-UHFFFAOYSA-N
Gene Information	human ... AR(367)

安全信息

象形图
警示用语：	Danger
危险声明	H351 - H360FD - H410
预防措施声明	P202 - P273 - P280 - P308 + P313 - P391 - P405
危险分类	Aquatic Chronic 1 - Carc. 2 - Repr. 1B
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

Y0001448

Bicalutamide for system suitability

European Pharmacopoeia (EP) Reference Standard

1861.35元/ ;

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产品说明

一般描述

生化/生理作用

包装

Unit quantity: 15 mg. Subject to change. The product is delivered as supplied by the issuing Pharmacopoeia. For the current unit quantity, please visit the EDQM reference substance catalogue.

注意

Please find SDS provided by EDQM here..

其他说明

Sales restrictions may apply.

基本信息

经验(实验)分子式	C₁₈H₁₄F₄N₂O₄S
分子量	430.37
MDL编号	MFCD00869971
PubChem化学物质编号	329831428
NACRES	NA.24

产品性质

等级	pharmaceutical primary standard
manufacturer/tradename	EDQM
application(s)	pharmaceutical (small molecule)
格式	neat
储存温度	2-8℃
SMILES string	CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc2ccc(C#N)c(c2)C(F)(F)F
InChI	1S/C18H14F4N2O4S/c1-17(26,10-29(27,28)14-6-3-12(19)4-7-14)16(25)24-13-5-2-11(9-23)15(8-13)18(20,21)22/h2-8,26H,10H2,1H3,(H,24,25)
InChI key	LKJPYSCBVHEWIU-UHFFFAOYSA-N
Gene Information	human ... AR(367)

安全信息

象形图
警示用语：	Danger
危险声明	H351 - H360FD - H410
预防措施声明	P202 - P273 - P280 - P308 + P313 - P391 - P405
危险分类	Aquatic Chronic 1 - Carc. 2 - Repr. 1B
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

B9061

Sigma-Aldrich

Bicalutamide (CDX)

≥98% (HPLC), powder

1682.59元/10 MG; 5343.25元/50 MG;

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产品说明

应用

比卡鲁胺已用作前列腺、膀胱癌细胞系和人胚胎骨骼肌细胞中的雄激素受体(AR)拮抗剂。它还被用作RPMI 1640 的补充剂，用于培养雄激素非依赖性LNCaP(LNCaP-AI)细胞系。

包装

10, 50 mg in glass bottle

生化/生理作用

特点和优势

这种化合物是基因调控研究的特色产品。点击此处发现更多特色基因调控产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。
这种化合物出现在《受体分类和信号转导手册》的核受体(类固醇)页面上。要浏览其他手册页，点击此处。
该化合物由AstraZeneca开发。要浏览其他药物开发化合物和批准的药物/候选药物列表，单击此处。

其他说明

斯克里普斯代谢组学和质谱技术中心独立生成的串联质谱数据可在PDF (B9061.pdf) 中查看或下载。斯克里普斯代谢物组学和质谱技术中心的METLIN代谢物数据库中有测试代谢物。要了解更多信息，请访问sigma.com/metlin。

基本信息

经验(实验)分子式	C₁₈H₁₄F₄N₂O₄S
分子量	430.37
MDL编号	MFCD00869971
PubChem化学物质编号	329773312
NACRES	NA.77

产品性质

质量水平	100
测定	≥98% (HPLC)
形式	powder
储存条件	desiccated protect from light
溶解性	DMSO: >5 mg/mL H₂O: insoluble
创始人	AstraZeneca
SMILES string	CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc2ccc(C#N)c(c2)C(F)(F)F
InChI	1S/C18H14F4N2O4S/c1-17(26,10-29(27,28)14-6-3-12(19)4-7-14)16(25)24-13-5-2-11(9-23)15(8-13)18(20,21)22/h2-8,26H,10H2,1H3,(H,24,25)
InChI key	LKJPYSCBVHEWIU-UHFFFAOYSA-N
Gene Information	human ... AR(367)

安全信息

象形图
警示用语：	Danger
危险声明	H351 - H360FD - H410
预防措施声明	P202 - P273 - P280 - P308 + P313 - P391 - P405
危险分类	Aquatic Chronic 1 - Carc. 2 - Repr. 1B
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable
个人防护装备	dust mask type N95 (US), Eyeshields, Gloves

BP1115

Bicalutamide

British Pharmacopoeia (BP) Reference Standard

2025.56元/100 MG;

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产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia. For further information and support please go to the website of the issuing Pharmacopoeia.

生化/生理作用

包装

Unit quantity: 100 mg. Subject to change. The product is delivered as supplied by the issuing Pharmacopoeia. For the current unit quantity please visit British Pharmacopoeia

其他说明

Sales restrictions may apply.

基本信息

经验(实验)分子式	C₁₈H₁₄F₄N₂O₄S
分子量	430.37
MDL编号	MFCD00869971
NACRES	NA.24

产品性质

等级	pharmaceutical primary standard
manufacturer/tradename	BP
格式	neat
储存温度	2-8℃
SMILES string	CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc2ccc(C#N)c(c2)C(F)(F)F
InChI	1S/C18H14F4N2O4S/c1-17(26,10-29(27,28)14-6-3-12(19)4-7-14)16(25)24-13-5-2-11(9-23)15(8-13)18(20,21)22/h2-8,26H,10H2,1H3,(H,24,25)
InChI key	LKJPYSCBVHEWIU-UHFFFAOYSA-N
Gene Information	human ... AR(367)

安全信息

象形图
警示用语：	Danger
危险声明	H351 - H360FD - H410
预防措施声明	P202 - P273 - P280 - P308 + P313 - P391 - P405
危险分类	Aquatic Chronic 1 - Carc. 2 - Repr. 1B
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable

1071202

USP

Bicalutamide

United States Pharmacopeia (USP) Reference Standard

3231.47元/200 MG;

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产品说明

一般描述

This product is provided as delivered and specified by the issuing Pharmacopoeia. All information provided in support of this product, including SDS and any product information leaflets have been developed and issued under the Authority of the issuing Pharmacopoeia.
For further information and support please go to the website of the issuing Pharmacopoeia.

生化/生理作用

分析说明

These products are for test and assay use only. They are not meant for administration to humans or animals and cannot be used to diagnose, treat, or cure diseases of any kind.

其他说明

Sales restrictions may apply.

基本信息

经验(实验)分子式	C₁₈H₁₄F₄N₂O₄S
分子量	430.37
MDL编号	MFCD00869971
PubChem化学物质编号	329749112
NACRES	NA.24

产品性质

等级	pharmaceutical primary standard
manufacturer/tradename	USP
application(s)	pharmaceutical (small molecule)
格式	neat
储存温度	2-8℃
SMILES string	CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc2ccc(C#N)c(c2)C(F)(F)F
InChI	1S/C18H14F4N2O4S/c1-17(26,10-29(27,28)14-6-3-12(19)4-7-14)16(25)24-13-5-2-11(9-23)15(8-13)18(20,21)22/h2-8,26H,10H2,1H3,(H,24,25)
InChI key	LKJPYSCBVHEWIU-UHFFFAOYSA-N
Gene Information	human ... AR(367)

安全信息

象形图
警示用语：	Danger
危险声明	H351 - H360FD - H410
预防措施声明	P202 - P273 - P280 - P308 + P313 - P391 - P405
危险分类	Aquatic Chronic 1 - Carc. 2 - Repr. 1B
储存分类代码	6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable