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经验公式（希尔记法）:
C18H14F4N2O4S
化学文摘社编号:
分子量:
430.37
NACRES:
NA.24
PubChem Substance ID:
UNSPSC Code:
41116107
MDL number:
产品名称
比卡鲁胺, European Pharmacopoeia (EP) Reference Standard
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)
SMILES string
CC(O)(CS(=O)(=O)c1ccc(F)cc1)C(=O)Nc2ccc(C#N)c(c2)C(F)(F)F
InChI key
LKJPYSCBVHEWIU-UHFFFAOYSA-N
grade
pharmaceutical primary standard
API family
bicalutamide
manufacturer/tradename
EDQM
application(s)
pharmaceutical (small molecule)
format
neat
storage temp.
2-8°C
Gene Information
human ... AR(367)
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Biochem/physiol Actions
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)。
比卡鲁胺(CDX)是一种非杀菌性雄激素受体 (AR) 拮抗剂，是一种纯雄激素抗体。
Application
Bicalutamide for system suitability EP Reference standard, intended for use in laboratory tests only as specifically prescribed in the European Pharmacopoeia.
General description
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.
Other Notes
Sales restrictions may apply.
Packaging
The product is delivered as supplied by the issuing Pharmacopoeia. For the current unit quantity, please visit the EDQM reference substance catalogue.
signalword
Danger
hcodes
Hazard Classifications
Aquatic Chronic 1 - Carc. 2 - Repr. 1B
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
P W Wong et al.
Chest, 113(2), 548-550 (1998-03-14)
A 69-year-old man with advanced prostate cancer was receiving antiandrogen therapy (bicalutamide [Casodex]). He developed dyspnea, peripheral eosinophilia and bilateral pulmonary interstitial infiltrates. Transbronchial biopsy confirmed pulmonary eosinophilia. Withdrawal of bicalutamide and initiation of steroid therapy resulted in clinical improvement.
Paul R Sieber
Expert review of anticancer therapy, 7(12), 1773-1779 (2007-12-08)
Bicalutamide is a competitive nonsteroidal androgen receptor antagonist. In the European Union and a number of other countries, bicalutamide 150 mg per day is approved as an adjuvant to primary treatments (radical prostatectomy or radiotherapy) or as monotherapy as an
High SPDEF may identify patients who will have a prolonged response to androgen deprivation therapy.
Andrew C Haller et al.
The Prostate, 74(5), 509-519 (2014-01-01)
Due to the indolent nature of prostate cancer, new prognostic measures are needed to identify patients with life threatening disease. SAM pointed domain-containing Ets transcription factor (SPDEF) has been associated with good prognosis and demonstrates an intimate relationship with the
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
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
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