Enzalutamide (MDV3100)

For research use only. Not for use in humans.

目录号:S1250

Enzalutamide (MDV3100) Chemical Structure

Molecular Weight(MW): 464.44

Enzalutamide (MDV3100)是一种androgen-receptor (AR)拮抗剂,在 LNCaP细胞中IC50为36 nM。研究证明 Enzalutamide 可促进自噬。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2444.41 现货
RMB 1221.51 现货
RMB 2224.43 现货
RMB 6297.61 现货
RMB 16298.1 现货
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产品安全说明书

Androgen Receptor抑制剂选择性比较

生物活性

产品描述 Enzalutamide (MDV3100)是一种androgen-receptor (AR)拮抗剂,在 LNCaP细胞中IC50为36 nM。研究证明 Enzalutamide 可促进自噬。
靶点
Androgen Receptor [1]
(LNCaP cells)
36 nM
体外研究

Enzalutamide是雄激素受体(AR)拮抗剂,IC50为36 nM。在加入16β-[18F]氟-5α-DHT (18-FDHT)的竞争性实验中发现作用于AR时Enzalutamide比bicalutamide具有更高的亲和力。而Enzalutamide作用于LNCaP/AR(AR-过量表达)前列腺细胞时没有效果。在亲本LNCaP细胞中,Enzalutamide抑制前列腺特异性抗原(PSA)和跨膜丝氨酸蛋白酶2(TMPRSS2) 的产生,及抑制它们与合成的雄激素R1881 结合。Enzalutamide可抑制突变AR蛋白(W741C, 741位上的Trp突变为Cys)的翻译活性。[1]MDV310也阻断核转位和配位受体复合物招募辅激活因子。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human LNCAP MlK2R5l1d3SxeHnjJGF{e2G7 NEnKR5g4KGSjeYO= MnzPPVUmKEW2T1i= NUTCeVkyUUN3ME21MlEzKM7:TR?= M2fsUVI{PzF|NU[3
human LNCAP NIizUIJHfW6ldHnvckBCe3OjeR?= MoOzNUDPxE1? M2HaTWROW09? MnKwTY5pcWKrdIOgdJJwe3SjdHWgd5Bm[2moaXOgZY51cWenbjDz[YNz\XSrb36gbY4hcHWvYX6gUG5ESVBiY3XscJMh\XiycnXzd4lv\yCjbnTyc4dmdiC{ZXPldJRweiCjdDCxNFAuOTByMH7N NWTEZWRnOjB{MUi3NVc>
VCaP MkHKSpVv[3Srb36gRZN{[Xl? NFPRT3EyOCEQvF2= NH\5XlgzPCCq M1S0W2ROW09? NESzepZUfXCycnXzd4V{KGyrZ3Hu[E1u\WSrYYTl[EBCWi2ITDDzbYdv[Wyrbneg NWfkVmpzOjJ5MUC0N|Y>
BCK4 Mn\xSpVv[3Srb36gRZN{[Xl? NHjQfJYyOCEQvF2= Mlv0O{Bl[Xm| NFzWcW9FVVOR MkLVTY5pcWKrdIOg[ZN1emGmaX;sMY1m\GmjdHXkJJBzd2yrZnXyZZRqd25? Mnz1NlQ1PTFzMEm=
MCF7s MV;GeY5kfGmxbjDBd5NigQ>? M3qyZlExKM7:TR?= M1ftXFYh\GG7cx?= M4fyfGROW09? M3PNd2lvcGmkaYTzJIV{fHKjZHnvcE1u\WSrYYTl[EBxem:uaX\ldoF1cW:w MYqyOFQ2OTFyOR?=
PC-3 NUC4fnVOTnWwY4Tpc44hSXO|YYm= Mo\hNVAh|ryP NIPMXos4OiCq NIjUVGFFVVOR MY\Ec4V{KG6xdDDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbh?= NITKeHgzPTN2NEi2OC=>
CWR22Rv1 NUHJWINRTnWwY4Tpc44hSXO|YYm= M1rpNFE2KM7:TR?= NXHO[4hiOjRiaB?= MofTSG1UVw>? NH3vc4xFd2W|IH7veEBi\m[nY4SgeIhmKG[3bHygcIVv\3SqIFHSJIV5eHKnc4Ppc44> NWfCdXFVOjN5MUO1Olc>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
AR / ERG / NOTCH1 / PSA / Cleaved PARP1 / Cleaved caspase 7; 

PubMed: 28607007     


Treatment of VCaP cells with NOTCH inhibitor, GSI-1, in combination with Enzalutamide (Enz) augmentes its effects on the inhibition of AR, ERG, PSA, NOTCH1 and NOTCH2 expression and induces cleavage of PARP1 and Caspase 7

AR-FL / AR-v7 / pAR(S213) / pAkt(S473) / pMdm2(S166); 

PubMed: 26378044     


LNCaP95 (LN95) cells were maintained in medium containing 5% CSS and then treated with 5μM of enzalutamide (ENZ) for 0-24 hours. Whole cell lyses were extracted. AR-FL, AR-v7, phosphor-AR(ser213), phosphorAkt(ser473), total Akt, total PP-1, phosphor-Mdm2(ser166), total Mdm2 and β-actin were measured by immunoblotting.

CXCR7; 

PubMed: 29277895     


Western blotting is used to analyze CXCR7 protein levels in VCaP and C4-2B cells.

28607007 26378044 29277895
Growth inhibition assay
Cell proliferation; 

PubMed: 28115200     


Proliferation of the LNCaP prostate cancer cell line, the Ramos Burkitt's cell line, and the Granta, Jeko-1, Rec-1 and Maver-1 MCL cell lines plated in charcoal stripped serum for 96 hours in the absence or presence of enzalutamide (10uM). Data are representative of 3 independent experiments.

28115200
Immunofluorescence
AR; 

PubMed: 27588408     


Representative immunofluorescent images show the expression and subcellular localization of AR in 22Rv1 cells overexpressing PIP5K1α that were treated with vehicle control, enzalutamide, ISA-2011B and combination of enzalutamide and ISA-2011B.

pAKT(S473); 

PubMed: 27588408     


Representative immunofluorescent images of subcellular localization of pAKT S473 expression in PC3 cells expressing AR-V7 that were treated with vehicle control (Ctrl), enzalutamide, ISA-2011B and combination of enzalutamide and ISA-2011B (ENZ+ISA2011B). The cancer cells are indicated by the arrows.

CXCR7; 

PubMed: 29277895     


Immunofluorescence staining is used to analyze CXCR7 protein levels in prostate cancer cells.

27588408 29277895
ELISA
osteoprotegerin; 

PubMed: 27015557     


MDA-MB-231 cells were treated with 10 μM enzalutamide or vehicle for 48 hours. Levels of OPG (osteoprotegerin) in the supernatant of MDA-MB-231 cells as determined by ELISA. Data are representative of 2 independent experiments.

27015557
体内研究 Enzalutamide处理携带LNCaP/AR移植瘤的阉割雄鼠,按鼠体重,每千克处理10mg MDV310,可诱导肿瘤的明显退化。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[3]
- 合并

AR受体实验:

在抗激素的前列腺癌细胞系中通过人工AR反应报告分子系统测定Enzalutamide。在这个系统中,前列腺癌LNCaP细胞稳定表达AR,表达的AR水平比体内自身产生的AR水平高5倍多。外界合成的AR和体内自身产生的AR有着相似的特性,都能稳定与合成的雄激素R1881作用。AR过量表达的细胞也能含有AR反应报告分子,这些细胞的报告分子活性显示抗激素前列腺癌的特性。在含100 pM R1881时测定Enzalutamide的抗性。LNCaP细胞供养在含有10%胎牛血清的Iscove's培养基中。在用Enzalutamide处理的前两天,细胞在含活性炭处理的胎牛血清(CS-FBS)Iscove's培养基中生长,用于除去雄激素。细胞在培养基上分裂和生长,培养基含有10% CS-FBS,100 pM R1881,及增加浓度的Enzalutamide。温育两天后,测定报告分子活性。
细胞实验:[1]
- 合并
  • Cell lines: LNCaP或LNCaP/AR细胞
  • Concentrations: 10 μM 左右
  • Incubation Time: 1-4天
  • Method: 用DMSO稀释Enzalutamide。LNCaP或LNCaP/AR细胞(104细胞/每孔)缺乏雄激素,在含有5-10%活性炭处理的血清培养基上生长3到5天。然后在5-10%活性炭处理的血清培养基中加入不同浓度(1到10000 nM)Enzalutamide处理细胞。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 雄激素非依赖性LNCaP/HR移植瘤雄性SCID鼠
  • Dosages: 10 mg/kg
  • Administration: 每天饲喂处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 92 mg/mL warmed (198.08 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
5% DMSO+1% CMC Na+1% Tween-80
17mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 464.44
化学式

C21H16F4N4O2S

CAS号 915087-33-1
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04335682 Not yet recruiting Drug: Darolutamide|Drug: Enzalutamide Metastatic Prostate Cancer|Prostate Cancer Metastatic|Prostate Cancer|Castrate Resistant Prostate Cancer Alliance Foundation Trials LLC.|Bayer May 2020 Phase 2
NCT03700099 Recruiting Drug: Docetaxel|Drug: Enzalutamide Prostate Cancer|Castration-resistant Prostate Cancer Instituto do Cancer do Estado de São Paulo|Astellas Pharma Inc September 3 2019 Phase 2
NCT03207529 Recruiting Drug: Alpelisib|Drug: Enzalutamide Advanced Breast Carcinoma|Anatomic Stage III Breast Cancer AJCC v8|Anatomic Stage IIIA Breast Cancer AJCC v8|Anatomic Stage IIIB Breast Cancer AJCC v8|Anatomic Stage IIIC Breast Cancer AJCC v8|Anatomic Stage IV Breast Cancer AJCC v8|Androgen Receptor Positive|HER2/Neu Negative|Metastatic Breast Carcinoma|Prognostic Stage III Breast Cancer AJCC v8|Prognostic Stage IIIA Breast Cancer AJCC v8|Prognostic Stage IIIB Breast Cancer AJCC v8|Prognostic Stage IIIC Breast Cancer AJCC v8|Prognostic Stage IV Breast Cancer AJCC v8|PTEN Positive|Recurrent Breast Carcinoma|Refractory Breast Carcinoma|Triple-Negative Breast Carcinoma M.D. Anderson Cancer Center|National Cancer Institute (NCI) June 7 2019 Phase 1

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常见问题及建议解决方法

  • 问题 1:

    I would like to inquire about the usage or solubility of S1250, Enzalutamide.

  • 回答:

    For in vivo experiment, S1250 can be dissolved in 2% DMSO+30% PEG 300+ddH2O at 5mg/ml as a suspension for oral gavage. And it can be dissolved in 15% DMSO+85% PEG 300 at 10mg/ml as a clear solution. When prepare the solution, please dissolve the compound in DMSO clearly first, then add PEG.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID