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Merck

Y0001448

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 for system suitability 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

危險聲明

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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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
Bicalutamide ('Casodex') development: from theory to therapy.
G J Kolvenbag et al.
The cancer journal from Scientific American, 3(4), 192-203 (1997-07-01)
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
J Anderson
Hospital medicine (London, England : 1998), 61(9), 660-663 (2000-10-26)
In men with locally advanced prostate cancer, bicalutamide 150 mg monotherapy provides a similar disease outcome to medical or surgical castration. However, castration is associated with loss of sexual interest and function, decreased energy and an increased risk of osteoporotic
K L Goa et al.
Drugs & aging, 12(5), 401-422 (1998-06-02)
Bicalutamide is a nonsteroidal antiandrogen with a long elimination half-life (t1/2) that permits once-daily administration. When combined with a gonadorelin (gonadotrophin releasing hormone; GnRH) agonist in maximum androgen blockade (MAB) regimens, bicalutamide 50 mg once daily is at least as

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