产品说明书

Enzalutamide

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Chemical Structure| 915087-33-1 同义名 : MDV3100
CAS号 : 915087-33-1
货号 : A270395
分子式 : C21H16F4N4O2S
纯度 : 98%
分子量 : 464.436
MDL号 : MFCD14155804
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(107.66 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 3 mg/mL clear

PO 0.5% CMC-Na 50 mg/mL suspension

生物活性
靶点

  • Androgen Receptor

    Androgen Receptor, IC50:36 nM
描述 The androgen receptor (AR), also known as NR3C4, is one kind of nuclear receptor. When binding either of androgenic hormones, testosterone or dihydrotestosterone, androgen receptor can be activated and translocate into the nucleus. Increased androgen receptor gene expression may critically influence cancer progression such as, prostate cancer[1]. Enzalutamide, also called as MDV3100, is an androgen-receptor (AR) antagonist with IC50 of 36 nM (measured by relative AR binding affinity)[1]. Enzalutamide can prevent nuclear translocation and impair DNA binding of AR induced by R1881 (a synthetic androgen)[1], which facilitated mediating reduced PSA levels in AR-positive prostate cancer cell line (LNCaP) and inhibiting the growth of LNCaP cells[3]. Enzalutamide is the first approved second-generation androgen receptor (AR) antagonist in the treatment of metastatic castration-resistant prostate cancer (mCRPC) and shows good pharmacokinetic profiles in human[4] as well as animal[5].
作用机制 Enzalutamide is a competitive inhibitor of AR ligand binding.[6]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
BCK4 10 μM Function Assay 7 days Inhibits estradiol-mediated proliferation 24451109
CWR22Rv1 15 μM Function Assay 24 h Does not affect the full length AR expression 23713567
human LNCAP Cytotoxic Assay 7 days IC50=5.12 μM 23713567
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01650194 Metastatic Castration-Resistan... 展开 >>t Prostate Cancer 收起 << Phase 2 Completed - United States, Texas ... 展开 >> Site US2492 MD Anderson Cancer Ctr Houston, Texas, United States, 77030 收起 <<
NCT03478904 Prostate Cancer Phase 1 Recruiting April 30, 2019 United States, Maryland ... 展开 >> National Institutes of Health Clinical Center Recruiting Bethesda, Maryland, United States, 20892 Contact: For more information at the NIH Clinical Center contact National Cancer Institute Referral Office    888-624-1937 收起 <<
NCT03305224 Castration-resistant Prostate ... 展开 >>Cancer Bone Metastases 收起 << Phase 2 Recruiting December 2019 Japan ... 展开 >> Osaka City University Graduate School of Medicine Recruiting Osaka, Japan, 545-8585 Contact: Taro Iguchi, MD, PhD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.77mL

2.15mL

1.08mL

21.53mL

4.31mL

2.15mL
参考文献

[1]Tran C, Ouk S, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science. 2009 May 8;324(5928):787-90.

[2]Saraon P, Jarvi K, et al. Molecular alterations during progression of prostate cancer to androgen independence. Clin Chem. 2011 Oct;57(10):1366-75.

[3]Ardiani A, Gameiro SR, et al. Androgen deprivation therapy sensitizes prostate cancer cells to T-cell killing through androgen receptor dependent modulation of the apoptotic pathway. Oncotarget. 2014 Oct 15;5(19):9335-48.

[4]Hong JH, et al. Pharmacokinetic/pharmacodynamic drug evaluation of enzalutamide for treating prostate cancer. Expert Opin Drug Metab Toxicol. 2018 Mar;14(3):361-369.

[5]Kim TH, Jeong JW, et al. Pharmacokinetics of enzalutamide, an anti-prostate cancer drug, in rats. Arch Pharm Res. 2015 Nov;38(11):2076-82.

[6]Golshayan AR, Antonarakis ES, et al. Enzalutamide: an evidence-based review of its use in the treatment of prostate cancer. Core Evid. 2013;8:27-35.