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Merck
CN

B9061

比卡鲁胺 (CDX)

≥98% (HPLC), non-steriodal Androgen Receptor (AR) Antagonist, 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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关于此项目

经验公式(希尔记法):
C18H14F4N2O4S
化学文摘社编号:
分子量:
430.37
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
protect from light
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产品名称

比卡鲁胺 (CDX), ≥98% (HPLC), powder

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

assay

≥98% (HPLC)

form

powder

storage condition

desiccated
protect from light

solubility

DMSO: >5 mg/mL
H2O: insoluble

originator

AstraZeneca

Quality Level

Gene Information

human ... AR(367)

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Application

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。

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。

Features and Benefits

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。

pictograms

Health hazardEnvironment

signalword

Danger

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

ppe

dust mask type N95 (US), Eyeshields, Gloves


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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S Belikov et al.
Molecular and cellular endocrinology, 365(1), 95-107 (2012-10-16)
Prostate cancer growth depends on androgens. Synthetic antiandrogens are used in the cancer treatment. However, antiandrogens, such as bicalutamide (BIC), have a mixed agonist/antagonist activity. Here we compare the antiandrogenic capacity of BIC to a new antiandrogen, MDV3100 (MDV) or
Maha Hussain et al.
The New England journal of medicine, 368(14), 1314-1325 (2013-04-05)
Castration resistance occurs in most patients with metastatic hormone-sensitive prostate cancer who are receiving androgen-deprivation therapy. Replacing androgens before progression of the disease is hypothesized to prolong androgen dependence. Men with newly diagnosed, metastatic, hormone-sensitive prostate cancer, a performance status
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
Testosterone insulin-like effects: an in vitro study on the short-term metabolic effects of testosterone in human skeletal muscle cells
Antinozzi C, et al.
Journal of Endocrinological Investigation, 40(10), 1133-1143 (2017)
Reactive stroma component COL6A1 is upregulated in castration-resistant prostate cancer and promotes tumor growth
Zhu YP, et al.
Testing, 6(16), 14488-14488 (2015)

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