Product Categories

MDV3100 (Enzalutamide)

MDV3100 is an androgen-receptor (AR) antagonist with IC50 of 36 nM.

Catalog No.S1250

2 Reviews 7 Product Citations

: Tel: +1-832-582-8158[email protected]

MDV3100 (Enzalutamide) Chemical Structure
Molecular Weight: 464.44

Validation & Quality Control

Product Citations(7)

Neoplasia, 2012, 14(1):74-83

Int J Cancer, 2012, 131(6), E872-883

Aging, 2013, ahead of print

Am J Pathol, 2013, 182(2):460-73

Mol Cell Endocrinol, 2013, 365(1), 95-107
PLoS One, 2012, 8(1), e53701

Prostate, 2012, ahead of print

Customer Reviews(2) in vivo invitation

PLoS One, 2013, 8(1), e53701. MDV3100 (Enzalutamide) purchased from Selleck

PLoS One, 2013, 8(1), e53701. MDV3100 (Enzalutamide) purchased from Selleck

Quality Control & MSDS

Related Compound Libraries

MDV3100 (Enzalutamide) is available in the following compound libraries:

Cambridge Cancer Compound Library(96-well) Chemical Library (96-well) Inhibitor Library (96-well)

Product Information

Compare CYP17 Inhibitors
Compare CYP17 Inhibitors
- Inhibitory Selectivity
- Solubility
Cat.No. Product Name Solubility (25°C)

Water DMSO Ethanol
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Product Description

Biological Activity Protocol Chemical Information Customer Reviews Product Citations Tech Support & FAQs

Biological Activity

Description	MDV3100 is an androgen-receptor (AR) antagonist with IC50 of 36 nM.
Targets	Androgen-receptor
IC50	36 nM ^[1]
In vitro	MDV3100 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 MDV3100 shows no agonism in LNCaP/AR prostate cells. MDV3100 antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. MDV3100 could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp⁷⁴¹ to Cys). ^[1] MDV3100 also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. ^[2]
In vivo	MDV3100 induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. ^[1]
Clinical Trials	MDV3100 is currently in Phase III clinical trial in progressive metastatic prostate cancer.
Features

Protocol(Only for Reference)

Kinase Assay: ^[3]

AR reporter assay	MDV3100 is evaluated by an artificial AR response reporter system in a hormone refractory prostate cancer cell line. In this system, the prostate cancer LNCaP cells are engineered to stably express about 5-fold higher level of AR than endogenous level. The exogenous AR has similar properties to endogenous AR in that both are stabilized by a synthetic androgen R1881. The AR-over expressed cells are also engineered to stably incorporate an AR response reporter and the reporter activity of these cells shows features of hormone refractory prostate cancer. The antagonistic activity of MDV3100 is tested in the presence of 100 pM of R1881. Engineered LNCaP cells are maintained in Iscove's medium containing 10% fetal bovine serum (FBS). Two days prior to MDV3100 treatment, the cells are grown in Iscove's medium containing 10% charcoal-stripped FBS (CS-FBS) to deprive of androgens. The cells are split and grown in Iscove's medium containing 10% CS-FBS with 100 pM of R1881 and increasing concentrations of MDV3100. After two days of incubation, reporter activities are assayed.

AR reporter assay

MDV3100 is evaluated by an artificial AR response reporter system in a hormone refractory prostate cancer cell line. In this system, the prostate cancer LNCaP cells are engineered to stably express about 5-fold higher level of AR than endogenous level. The exogenous AR has similar properties to endogenous AR in that both are stabilized by a synthetic androgen R1881. The AR-over expressed cells are also engineered to stably incorporate an AR response reporter and the reporter activity of these cells shows features of hormone refractory prostate cancer. The antagonistic activity of MDV3100 is tested in the presence of 100 pM of R1881. Engineered LNCaP cells are maintained in Iscove's medium containing 10% fetal bovine serum (FBS). Two days prior to MDV3100 treatment, the cells are grown in Iscove's medium containing 10% charcoal-stripped FBS (CS-FBS) to deprive of androgens. The cells are split and grown in Iscove's medium containing 10% CS-FBS with 100 pM of R1881 and increasing concentrations of MDV3100. After two days of incubation, reporter activities are assayed.

Cell Assay: ^[1]

Cell lines	LNCaP or LNCaP/AR cells
Concentrations	0-10 μM
Incubation Time	1-4 days
Method	MDV3100 is diluted in DMSO. LNCaP or LNCaP/AR cells (10⁴ cells/well) are androgen-starved by growth in media containing 5-10% charcoal-stripped serum for 3-5 days. Then the cells are challenged with various concentrations of MDV3100 in media containing 5-10% charcoal-stripped serum.

Animal Study: ^[1]

Animal Models	Castration-resistant LNCaP/HR xenografts in male SCID mice
Formulation	Formulated in 1% carboxymethyl cellulose, 0.1% Tween-80, 5% DMSO
Dosages	10 mg/kg
Administration	Administered via gavage daily

References

Chemical Information

Download MDV3100 (Enzalutamide) SDF

Molecular Weight (MW)	464.44
Formula	C₂₁H₁₆F₄N₄O₂S
CAS No.	915087-33-1
Synonyms	N/A

Solubility (25°C) DMSO 93 mg/mL Water <1 mg/mL Ethanol 3 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name

Molarity Calculator Dilution Calculator Molecular Weight Calculator

Research Area

Customer Reviews (2)

Click to enlarge

Rating

Source

PLoS One, 2013, 8(1), e53701. MDV3100 (Enzalutamide) purchased from Selleck

Method

Western blots/qPCR

Cell Lines

CWR-R1 cells

Concentrations

10 μM

Incubation Time

48 h

Results

MDV3100 treatment reverses androgen-mediated decreases of Sox2 protein and mRNA in CWR-R1 cells 48 hours after a 24 hour pretreatment with R1881.

Click to enlarge

Rating

Source

PLoS One, 2013, 8(1), e53701. MDV3100 (Enzalutamide) purchased from Selleck

Method

qPCR

Cell Lines

prostate cancer cell lines

Concentrations

10 μM

Incubation Time

30 d

Results

There is a significant decrease in PSA expression under continuous AR inhibition with MDV3100.

Product Citations (7)

ASC-J9 suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors. [Yamashita S, et al. Neoplasia 2012;14(1):74-83]
PubMed: 22355276
Distinct expression and activity of GSK-3α and GSK-3β in prostate cancer. [Darrington RS, et al. Int J Cancer 2012;131(6), E872-883]
PubMed: 22539113
Structural and functional association of androgen receptor with telomeres in prostate cancer cells. [Zhou J, et al. Aging 2013;ahead of print]
PubMed: 23363843

New Therapeutic Approach to Suppress Castration-Resistant Prostate Cancer Using ASC-J9 via Targeting Androgen Receptor in Selective Prostate Cells. [Lai KP, et al. Am J Pathol 2013;182(2):460-73]
PubMed: 23219429
FoxA1 corrupts the antiandrogenic effect of bicalutamide but only weakly attenuates the effect of MDV3100 (Enzalutamide™). [Belikov S, et al. Mol Cell Endocrinol 2013;365(1), 95-107]
PubMed: 23063623
Sox2 is an androgen receptor-repressed gene that promotes castration-resistant prostate cancer. [Kregel S, et al. PLoS One 2012;8(1), e53701]
PubMed: 23326489
Growth kinetics of CD133-positive prostate cancer cells. [Reyes EE, et al. Prostate 2012;ahead of print]
PubMed: 23138940

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related CYP17 Inhibitors

Andarine (GTX-007)
Andarine (GTX-007) is a selective nonsteroidal androgen receptor (AR) agonist with K_i of 4 nM.
Ostarine(MK-2866)
Ostarine (GTx-024, MK-2866, Enobosarm, S-22) is a selective androgen receptor modulator (SARM) with K_i of 3.8 nM.
TAK-700 (Orteronel)
TAK-700 (Orteronel) is a potent and highly selective rat and human 17,20-lyase inhibitor with IC50 of 54 nM and 38 nM, respectively.
Cyproterone acetate
Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM.
Avasimibe(CI-1011)
Avasimibe inhibits ACAT and CYP2C9 with IC50 of 3.3 μM and 2.9 μM, respectively.
Alizarin
Alizarin strongly inhibits P450 isoform CYP1A1, CYP1A2 and CYP1B1 with IC50 of 6.2 μM, 10.0 μM and 2.7 μM, respectively.
TH-302
TH-302 is selective hypoxia-activated prodrug targeting hypoxic regions of solid tumors with IC50 of 19 nM.
Galeterone (TOK-001)
Galeterone (TOK-001, VN/124-1) is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively.
PF-4981517
PF-4981517 is a potent and selective inhibitor of CYP3A4 (P450) with IC50 of 0.03 μM.
Varespladib (LY315920)
LY315920 (Varespladib) is a potent and selective secretory phospholipase A2 (sPLA) inhibitor with IC50 of 7 nM.

Choose Your Country or Region

Product Categories

MDV3100 (Enzalutamide)