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B9061

Sigma-Aldrich

比卡鲁胺 (CDX)

≥98% (HPLC), powder

别名:

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:
90357-06-5
分子量:
430.37
MDL號碼:
MFCD00869971
分類程式碼代碼:
12352200
PubChem物質ID:
329773312
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

儲存條件

desiccated
protect from light

溶解度

DMSO: >5 mg/mL
H2O: insoluble

起源

AstraZeneca

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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應用

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。

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)。

特點和優勢

该化合物是受体分类及信号转导手册上核受体（类固醇）页面上的特色化合物。想要浏览手册的其他页面， 请单击此处。
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。
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。

象形圖

Health hazardEnvironment
GHS08,GHS09

訊號詞

Danger

危險聲明

H351,H360FD,H410

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

個人防護裝備

dust mask type N95 (US), Eyeshields, Gloves

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Paucity of PD-L1 expression in prostate cancer: innate and adaptive immune resistance
Martin AM, et al.
Prostate Cancer and Prostatic Diseases, 18(4), 325-325 (2015)
Androgen receptor antagonist bicalutamide induces autophagy and apoptosis via ULK2 upregulation in human bladder cancer cells
Hao K, et al.
International Journal of Clinical and Experimental Pathology, 10(7), 7603-7615 (2017)
Harald Bull Ragnum et al.
International journal of radiation oncology, biology, physics, 87(4), 753-760 (2013-09-17)
We explored changes in hypoxia-inducible factor 1 (HIF1) signaling during androgen deprivation therapy (ADT) of androgen-sensitive prostate cancer xenografts under conditions in which no significant change in immunostaining of the hypoxia marker pimonidazole had occurred. Gene expression profiles of volume-matched
Päivi Östling et al.
Cancer research, 71(5), 1956-1967 (2011-02-24)
Androgen receptor (AR) is expressed in all stages of prostate cancer progression, including in castration-resistant tumors. Eliminating AR function continues to represent a focus of therapeutic investigation, but AR regulatory mechanisms remain poorly understood. To systematically characterize mechanisms involving microRNAs
Benoît Boutin et al.
The Prostate, 73(10), 1090-1102 (2013-03-28)
Treatment of advanced prostate cancer (PCa) relies on pharmacological or surgical androgen deprivation. However, it is only temporarily efficient. After a few months or years, the tumor relapses despite the absence of androgenic stimulation: a state referred to as hormone-refractory
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