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/ Enzalutamide/恩杂鲁胺

Enzalutamide/恩杂鲁胺 {[allProObj[0].p_purity_real_show]}

货号：A270395 同义名： MDV3100

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。

Enzalutamide/恩杂鲁胺 化学结构 CAS号：915087-33-1
Enzalutamide/恩杂鲁胺 化学结构
CAS号：915087-33-1
Enzalutamide/恩杂鲁胺 3D分子结构
CAS号：915087-33-1
Enzalutamide/恩杂鲁胺 化学结构 CAS号：915087-33-1
Enzalutamide/恩杂鲁胺 3D分子结构 CAS号：915087-33-1
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Enzalutamide/恩杂鲁胺 纯度/质量文件 产品仅供科研

货号：A270395 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
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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

 		99%
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%
Spironolactone ++

Androgen Receptor, IC50: 77 nM

 		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。

Enzalutamide/恩杂鲁胺 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]

Enzalutamide/恩杂鲁胺 细胞实验

Cell Line
Concentration Treated Time Description References
Myc-CaP cells 50 µM >12 months To generate Enzalutamide-resistant cell lines, it was found that immune-related signaling pathways were suppressed in resistant cells J Immunother Cancer. 2023 May;11(5):e006581.
C4-2B cells 20 µM To study the mechanisms of Enzalutamide resistance, it was found that immune-related signaling pathways were suppressed in resistant cells J Immunother Cancer. 2023 May;11(5):e006581.
PC-3 10 μΜ 5 days Enzalutamide treatment did not induce senescence in PC-3 cells but increased CDC6 levels. J Exp Clin Cancer Res. 2023 Jul 29;42(1):187.
C4-2B 10 μΜ 5 days Enzalutamide treatment did not induce senescence in C4-2B cells but increased CDC6 levels. J Exp Clin Cancer Res. 2023 Jul 29;42(1):187.
LNCaP 10 μΜ 5 days Enzalutamide treatment induced senescence in LNCaP cells via reduction of the replication licensing factor CDC6. J Exp Clin Cancer Res. 2023 Jul 29;42(1):187.
CWR22Rv1 cells 20 μM 3 and 5 days To evaluate the combined inhibitory effect of Enzalutamide and Niclosamide on CWR22Rv1 cells, the results showed significant growth inhibition with the combination treatment. Clin Cancer Res. 2014 Jun 15;20(12):3198-3210.
C4-2B MR cells 20 μM 48 h To evaluate the inhibitory effect of Enzalutamide on C4-2B MR cells, the results showed limited growth inhibition of C4-2B MR cells by Enzalutamide. Clin Cancer Res. 2014 Jun 15;20(12):3198-3210.
VCaP cells 5 µM 48 h To investigate the effect of ROR-γ antagonists on AR-V7 gene expression, results showed that XY018 and SR2211 significantly inhibited AR-V7 gene expression. Nat Med. 2016 May;22(5):488-96.
C4-2B cells 5 µM 48 h To investigate the effect of ROR-γ antagonists on AR gene expression, results showed that SR2211 significantly inhibited AR gene expression. Nat Med. 2016 May;22(5):488-96.

Enzalutamide/恩杂鲁胺 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
FVB mice Myc-CaP tumor model Oral 25 mg/kg 5 days per week for 2 weeks To study the effects of Enzalutamide on immune cells in the tumor microenvironment, it was found that Enzalutamide treatment decreased CD8+ T-cell numbers and increased M-MDSC and PD-L1 expression J Immunother Cancer. 2023 May;11(5):e006581.
SCID mice LNCaP and C4-2B xenograft models Oral gavage 10 mg/kg 8 consecutive days Enzalutamide treatment induced senescence in LNCaP xenografts, reduced CDC6 levels, increased p21WAF1/Cip1 expression, and attenuated EMT. In C4-2B xenografts, Enzalutamide treatment did not induce senescence but increased CDC6 levels and EMT activity. J Exp Clin Cancer Res. 2023 Jul 29;42(1):187.
SCID mice CWR22Rv1 tumor model Oral 25 mg/kg 3 weeks To evaluate the combined inhibitory effect of Enzalutamide and Niclosamide on CWR22Rv1 tumors, the results showed significant tumor growth inhibition with the combination treatment. Clin Cancer Res. 2014 Jun 15;20(12):3198-3210.
Mice C4-2B xenograft model Intraperitoneal injection 5 mg/kg 5 times a week for 24 days To investigate the effect of SR2211 on tumor growth in the C4-2B xenograft model, results showed that SR2211 significantly inhibited tumor growth. Nat Med. 2016 May;22(5):488-96.
Mice Ptenpc-/- mice Oral 30 mg/kg Daily for 12 weeks Anti-IL23 treatment can reverse castration resistance in prostate cancer and enhance the efficacy of ENZA. Nature. 2018 Jul;559(7714):363-369

Enzalutamide/恩杂鲁胺 动物研究

Dose Mice: min = 10 mg/kg[7], max = 60 mg/kg[8]
Administration p.o.

Enzalutamide/恩杂鲁胺 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 <<

Enzalutamide/恩杂鲁胺 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.

Enzalutamide/恩杂鲁胺 实验方案

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

Enzalutamide/恩杂鲁胺 技术信息

CAS号915087-33-1
分子式C21H16F4N4O2S
分子量 464.44
SMILES Code CC1(C(N(C(N1C2=CC(F)=C(C(NC)=O)C=C2)=S)C3=CC(C(F)(F)F)=C(C#N)C=C3)=O)C
MDL No. MFCD14155804
别名 MDV3100
运输蓝冰
InChI Key WXCXUHSOUPDCQV-UHFFFAOYSA-N
Pubchem ID 15951529
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature
溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Enzalutamide | MDV3100 | Androgen Receptor | AmBeed-信号通路专用抑制剂 | Enzalutamide/恩杂鲁胺 纯度/质量文件 | Enzalutamide/恩杂鲁胺 亚型比较 | Enzalutamide/恩杂鲁胺 生物活性 | Enzalutamide/恩杂鲁胺 动物研究 | Enzalutamide/恩杂鲁胺 临床数据 | Enzalutamide/恩杂鲁胺 参考文献 | Enzalutamide/恩杂鲁胺 实验方案 | Enzalutamide/恩杂鲁胺 技术信息

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