Enzalutamide (MDV3100) - Moligand™, 10mM in DMSO , Androgen Receptor antagonist, CAS No.915087-33-1, Androgen Receptor antagonist

CAS: 915087-33-1 Cat. No.: E407899 Molecular Weight: 464.44 EC Number: 805-022-1

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

4-​[3-​[4-​cyano-​3-​(trifluoromethyl)​phenyl]​-​5,​5-​dimethyl-​4-​oxo-​2-​thioxo-​1-​imidazolidinyl]​-​2-​fluoro-​N-​methyl-benzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Enzalutamide (MDV3100) Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy .
In vitro

Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-[¹⁸F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp⁷⁴¹ to Cys). Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex.

In vivo

Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg.
Cell Data

cell lines：

Concentrations：0-10 μM

Incubation Time：1-4 days

Powder Purity:≥99%

Specifications

Synonyms

4-​[3-​[4-​cyano-​3-​(trifluoromethyl)​phenyl]​-​5, ​5-​dimethyl-​4-​oxo-​2-​thioxo-​1-​imidazolidinyl]​-​2-​fluoro-​N-​methyl-benzamide

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ANTAGONIST

Mechanism of action

Androgen Receptor antagonist

Product Properties

• ALogP: 3.6

Names and Identifiers

• Isomeric SMILES: CC1(C(=O)N(C(=S)N1C2=CC(=C(C=C2)C(=O)NC)F)C3=CC(=C(C=C3)C#N)C(F)(F)F)C
• Alternate CAS: 915087-33-1
• MeSH Entry Terms: 4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl)-2-fluoro-N-(methyl-d3)benzamide;4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxo-1-imidazolidinyl)-2-fluoro-N-methyl-benzamide;enzalutamide;enzaluta
• Molecular Weight: 464.44
• Reaxy-Rn: 11718700
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11718700&ln=

Associated Targets(Human)

KLK3 Tclin Prostate-specific antigen (1 Activities)

Discover Target: KLK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AR Tclin Androgen receptor (12 Activities)

Discover Target: AR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

References

1. Jiang Zhihui, Zhou Bo, Li Xinping, Kirby Gordon M., Zhang Xiaoying.  (2018)  Echinacoside Increases Sperm Quantity in Rats by Targeting the Hypothalamic Androgen Receptor.  Scientific Reports,  8  (1): (1-11).  [PMID:29497114] [10.1038/s41598-018-22211-1]

2. Shijia Lu, Chenxiao Zhang, Huiru Wu, Junjie Wang, Jinglong Wang, Limei Zhao, Tianyang Ren, Guofei Li.  (2025)  A pH/MMP-9 smart dual-responsive liposome GBE@LP co-delivers and controls the release of GB1107/BMS1166/Enzalutamide for liver cancer immunotherapy.  Materials Today Bio,      [PMID:40475856] [10.1016/j.mtbio.2025.101801]

3. Tingting Zheng, Hang Yin, Hongna Shan, Lihuan Sun, Lili Jiang, Yong Liu.  (2025)  Synergistic inhibitory effects of enzalutamide and its phase I metabolite on UDP-glucuronosyltransferase 1A1 (UGT1A1) and risk prediction of drug-drug interactions.  CHEMICO-BIOLOGICAL INTERACTIONS,      [PMID:41241169] [10.1016/j.cbi.2025.111829]