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Merck

Y0001444

比卡鲁胺

European Pharmacopoeia (EP) Reference Standard

别名:

比卡鲁胺 (CDX), N-[4-氰基-3-(三氟甲基)苯基]-3-(4-氟苯硫酰基)-2-甲基-2-羟基丙酰胺, 比卡他胺, 比卡胺

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About This Item

经验公式(希尔记法):
C18H14F4N2O4S
CAS号:
分子量:
430.37
MDL號碼:
分類程式碼代碼:
41116107
PubChem物質ID:
NACRES:
NA.24

等級

pharmaceutical primary standard

API 家族

bicalutamide

製造商/商標名

EDQM

應用

pharmaceutical (small molecule)

格式

neat

儲存溫度

2-8°C

SMILES 字串

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 密鑰

LKJPYSCBVHEWIU-UHFFFAOYSA-N

基因資訊

human ... AR(367)

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一般說明

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.

應用

Bicalutamide EP Reference standard, intended for use in laboratory tests only as specifically prescribed in the European Pharmacopoeia.

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)。

包裝

The product is delivered as supplied by the issuing Pharmacopoeia. For the current unit quantity, please visit the EDQM reference substance catalogue.

其他說明

Sales restrictions may apply.

象形圖

Health hazardEnvironment

訊號詞

Danger

危險分類

Aquatic Chronic 1 - Carc. 2 - Repr. 1B

儲存類別代碼

6.1C - Combustible, acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Wiebke Hessenkemper et al.
Molecular endocrinology (Baltimore, Md.), 28(11), 1831-1840 (2014-09-10)
We have previously identified a natural occurring, androgen receptor-specific antagonist. Atraric acid (AA) inhibits the transactivation of the androgen receptor (AR) and androgen-mediated growth of AR-expressing human prostate cancer (PCa) cell lines. Here we show that AA treatment of living
Brian D Lehmann et al.
Breast cancer research : BCR, 16(4), 406-406 (2014-08-12)
Triple negative breast cancer (TNBC) is a heterogeneous collection of biologically diverse cancers, which contributes to variable clinical outcomes. Previously, we identified a TNBC subtype that has a luminal phenotype and expresses the androgen receptor (AR+). TNBC cells derived from
Keri Wellington et al.
Drugs, 66(6), 837-850 (2006-05-19)
Bicalutamide (Casodex) is a competitive androgen receptor antagonist that inactivates androgen-regulated prostate cell growth and function, leading to cell apoptosis and inhibition of prostate cancer growth. It is administered orally as a once-daily dose. In the EU and a number
Ian D Cockshott
Clinical pharmacokinetics, 43(13), 855-878 (2004-10-29)
Bicalutamide is a nonsteroidal pure antiandrogen given at a dosage of 150 mg once daily as monotherapy for the treatment of early (localised or locally advanced) nonmetastatic prostate cancer. It is used at a dosage of 50 mg once daily
G J Kolvenbag et al.
The Prostate, 34(1), 61-72 (1998-01-15)
Bicalutamide (Casodex) is a new nonsteroidal antiandrogen developed for use in patients with prostate cancer. The efficacy and tolerability of bicalutamide as monotherapy and as combination therapy for patients with advanced prostate cancer have been evaluated in randomized clinical trials.

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