Enzalutamide(MDV3100) 是一种雄激素受体 (AR) 拮抗剂,在 LNCaP 前列腺细胞中的 IC50 为 36 nM。它还可以激活自噬。
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产品名称 | Androgen Receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Cyproterone acetate |
++++
Androgen Receptor, IC50: 7.1 nM |
98% | |||||||||||||||||
Apalutamide |
+++
Androgen Receptor, IC50: 16 nM |
98% | |||||||||||||||||
AZD3514 |
+
Androgen Receptor, Ki: 2.2 μM |
98% | |||||||||||||||||
Darolutamide |
++++
Androgen receptor, Ki: 11 nM |
98% | |||||||||||||||||
Flutamide |
+++
Androgen Receptor, Ki: 55 nM |
98% | |||||||||||||||||
Galeterone |
++
Androgen Receptor, IC50: 384 nM |
98% | |||||||||||||||||
Enzalutamide |
+++
Androgen Receptor, IC50: 36 nM |
98% | |||||||||||||||||
Megestrol | ✔ | 98% | |||||||||||||||||
Bicalutamide |
++
Androgen Receptor, IC50: 0.16 μM |
99% | |||||||||||||||||
EPI-001 |
+
Androgen Receptor, IC50: ~6 μM |
98% | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
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 | |
human LNCAP | 1 μM | Function Assay | Inhibits prostate specific antigen secretion in human LNCAP cells expressing androgen receptor at 100-1000nM | 20218717 | |
Dose | Mice: min = 10 mg/kg[7], max = 60 mg/kg[8] |
Administration | p.o. |
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 << |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 915087-33-1 |
分子式 | C21H16F4N4O2S |
分子量 | 464.436 |
别名 | MDV3100 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
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 |