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Enzalutamide

Enzalutamide

产品编号 T6002   CAS 915087-33-1
别名: MDV3100, 恩杂鲁胺

Enzalutamide (MDV3100) 是一种雄激素受体 (AR) 拮抗剂 (IC50=36 nM in LNCaP)。Enzalutamide 可以激活自噬,具有抗肿瘤活性,常用于去势抵抗性前列腺癌的治疗。

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Enzalutamide Chemical Structure
Enzalutamide, CAS 915087-33-1
规格 价格/CNY 货期 数量
1 mg ¥ 233 现货
5 mg ¥ 536 现货
10 mg ¥ 863 现货
25 mg ¥ 1,550 现货
50 mg ¥ 2,580 现货
100 mg ¥ 3,770 现货
200 mg ¥ 5,320 现货
500 mg ¥ 7,780 现货
1 g ¥ 9,820 现货
2 g ¥ 13,500 现货
1 mL * 10 mM (in DMSO) ¥ 645 现货
其他形式的 Enzalutamide:
产品目录号及名称: Enzalutamide (T6002)
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选择批次  
纯度: 100%
纯度: 99.67%
纯度: 99.48%
纯度: 99%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP). Enzalutamide activates autophagy, has antitumor activity, and is commonly used in the treatment of desmoplasia-resistant prostate cancer.
靶点活性 Androgen receptor:36 nM (LNCaP cells)
体外活性 方法:人前列腺癌细胞 LNCaP、PC3 和人骨肉瘤细胞 SJSA-1 用 Enzalutamide (0.01-100 μM) 处理 1 h,使用 MTT 检测细胞活力。
结果:Enzalutamide 显示降低了所有细胞系的生存能力,对 LNCaP、PC3 和 SJSA-1 细胞系的 LD50 分别为 12 μM、23.4 μM 和 34.7 μM。[1]
方法:人前列腺癌细胞 VCaP 用 Enzalutamide (10 μM) 处理 1-3 天,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:Enzalutamide 上调 cleaved-PARP 表达,诱导细胞凋亡。[2]
体内活性 方法:为检测体内抗肿瘤活性,将 Enzalutamide (1-50 mg/kg) 灌胃给药给携带人去势抵抗性肿瘤 (CRPC) LNCaP-AR-Lux 的 CB17SCID 小鼠,每天一次,持续二十八天。
结果:Enzalutamide 在 CRPC 异种移植物模型中诱导肿瘤体积的消退,并在 AR 过度扩张的前列腺癌症细胞中诱导细胞凋亡。[3]
方法:为评估 AR 在性成熟后骨代谢和骨骼生长中的作用,将 Enzalutamide (10-100 mg/kg,1% carboxymethyl cellulose+0.5% Tween 80+5% dimethylsulfoxide) 口服给药给 C57BL/6N 小鼠,每天一次,持续二十一天。
结果:Enzalutamide 降低了轴骨中的骨量,Enzalutamide 显著降低了轴心骨骼的机械强度。性成熟后,Enzalutamide 可减少雄性小鼠中轴骨骼的骨量,但不能减少阑尾骨骼的骨量。[4]
细胞实验 For in vitro experiments, LNCaP or LNCaP/AR cells (10^4 cells/well) were androgen-starved by growth in media containing 5-10% charcoal-stripped serum for 3-5 days. Then the cells were challenged with various concentrations of R1881, bicalutamide, RD162 or MDV3100 in media containing 5-10% charcoal-stripped serum [1].
动物实验 In vivo tumorigenicity experiments were done by subcutaneous injection of 10^6 cells (100 uL in 50% Matrigel and 50% growth media) into the flanks of castrated male SCID mice. Daily gavage treatment (using a formulation of 1% carboxymethyl cellulose, 0.1% Tween-80, 5% DMSO) was initiated when tumor size reached ~100 mm3. Tumor size was measured weekly in three dimensions (l x w x d) with calipers. For in vivo luciferase imaging, d-luciferin substrate (100 μL, 15 mg/mL) was injected intraperitoneally. After 5 minutes, mice were anesthetized using isofluorane and imaged using a cooled charged-coupled device IVIS camera. Data were analyzed using Living Image 2.30 software [1].
别名 MDV3100, 恩杂鲁胺
分子量 464.44
分子式 C21H16F4N4O2S
CAS No. 915087-33-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 85 mg/mL (183 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1531 mL 10.7657 mL 21.5313 mL 53.8283 mL
5 mM 0.4306 mL 2.1531 mL 4.3063 mL 10.7657 mL
10 mM 0.2153 mL 1.0766 mL 2.1531 mL 5.3828 mL
20 mM 0.1077 mL 0.5383 mL 1.0766 mL 2.6914 mL
50 mM 0.0431 mL 0.2153 mL 0.4306 mL 1.0766 mL
100 mM 0.0215 mL 0.1077 mL 0.2153 mL 0.5383 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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参考文献

1. Wright TC, et al. Abiraterone In Vitro Is Superior to Enzalutamide in Response to Ionizing Radiation. Front Oncol. 2021 Jul 21;11:700543. 2. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009 May 8;324(5928):787-90. 3. Guerrero J, et al. Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration-resistant prostate cancer. Prostate. 2013 Sep;73(12):1291-305. 4. Wu J, et al. Enzalutamide Reduces the Bone Mass in the Axial But Not the Appendicular Skeleton in Male Mice. Endocrinology. 2016 Feb;157(2):969-77.

文献引用

1. Sun R, Yan B, Li H, et al.Androgen receptor variants confer castration resistance in prostate cancer by counteracting antiandrogen-induced ferroptosis.Cancer Research.2023 2. Shi F, Wu L, Cui D, et al.LncFALEC recruits ART5/PARP1 and promotes castration-resistant prostate cancer through enhancing PARP1-meditated self PARylation.Cellular Oncology.2023: 1-16. 3. Ren L, Luo H, Zhao J, et al.An integrated in vitro/in silico approach to assess the anti-androgenic potency of isobavachin.Food and Chemical Toxicology.2023: 113764. 4. Zhao J, Sun Y, Ren L, et al.Antagonism of androgen receptor signaling by aloe-emodin.Food and Chemical Toxicology.2023: 114092. 5. Ekiciler A, Chen W L K, Bo Y, et al.Quantitative Cytochrome P450 3A4 Induction Risk Assessment Using Human Hepatocytes Complemented with Pregnane X Receptor-Activating Profiles.Drug Metabolism and Disposition.2023, 51(3): 276-284. 6. Pan W, Zhang Z, Kimball H, et al. Abiraterone acetate induces CREB1 phosphorylation and enhances the function of the CBP-p300 complex, leading to resistance in prostate cancer cells. Clinical Cancer Research. 2021, 27(7): 2087-2099. 7. Ghoochani A, Hsu E C, Aslan M, et al. Ferroptosis inducers are a novel therapeutic approach for advanced prostate cancer. Cancer research. 2021 Mar 15;81(6):1583-1594. doi: 10.1158/0008-5472.CAN-20-3477. Epub 2021 Jan 22. 8. Liu S, Tao Y, Wu S, et al.Sanguinarine chloride induces ferroptosis by regulating ROS/BACH1/HMOX1 signaling pathway in prostate cancer.Chinese Medicine.2024, 19(1): 1-18. 9. Tao Y, Lu J, Li L, et al.Raltitrexed induces apoptosis through activating ROS-mediated ER stress by impeding HSPA8 expression in prostate cancer cells.Biochimica et Biophysica Acta (BBA)-Molecular Cell Research.2024: 119684.
Lasalocid sodium AZD-8055 Cyclovirobuxine D Peretinoin Dactolisib Indomethacin β-Lapachone Ridaforolimus

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌药物库 抗癌活性化合物库 抗癌上市药物库 经典已知活性库 抗癌化合物库 已知活性化合物库 抗肝癌化合物库 含氟化合物库 抗前列腺癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Enzalutamide 915087-33-1 Autophagy Endocrinology/Hormones Androgen Receptor LNCaP prostate cell MDV3100 Inhibitor 恩杂鲁胺 MDV-3100 MDV 3100 inhibit inhibitor

 

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