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Enzalutamide (MDV3100)

Enzalutamide (MDV3100)

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

Kinase Assay: ^[3]

Cell Assay: ^[1]

Animal Study: ^[1]

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

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Kinase Assay: ^[3]

Cell Assay: ^[1]

Animal Study: ^[1]

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

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Kinase Assay: [3]

Cell Assay: [1]

Animal Study: [1]

References

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Kinase Assay: ^[3]

Cell Assay: ^[1]

Animal Study: ^[1]

Int J Cancer,2012, 131(6):E872-83

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

Aging,2013, 5(1):3-17

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

Mol Cell Endocrinol,2013, 365(1):95-107
Prostate,2012, 73(7):724-33

PLoS One,2013, 8(5):e63466

PLoS One,2012, 8(1):e53701

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

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

Inhibitor Library Bioactive Compound Library Cambridge Cancer Compound Library

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

Cat.No.	Product Name	Solubility (25°C)
S1250	Enzalutamide (MDV3100)	<1 mg/mL	93 mg/mL	<1 mg/mL
S1190	Bicalutamide	<1 mg/mL	86 mg/mL	5 mg/mL
S2840	ARN-509	<1 mg/mL	18 mg/mL	5 mg/mL
S1174	MK-2866 (GTx-024)	<1 mg/mL	78 mg/mL	78 mg/mL
S1908	Flutamide	<1 mg/mL	55 mg/mL	55 mg/mL
S2042	Cyproterone Acetate	<1 mg/mL	83 mg/mL	10 mg/mL
S1140	Andarine	<1 mg/mL	88 mg/mL	88 mg/mL
S2803	Galeterone	<1 mg/mL	24 mg/mL	40 mg/mL
S1304	Megestrol Acetate	<1 mg/mL	33 mg/mL	15 mg/mL
S4054	Spironolactone	<1 mg/mL	83 mg/mL	20 mg/mL
S7040	AZD3514	<1 mg/mL	100 mg/mL	100 mg/mL

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

AR reporter assay	Enzalutamide 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 Enzalutamide 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 Enzalutamide 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 Enzalutamide. After two days of incubation, reporter activities are assayed.

AR reporter assay

Enzalutamide 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 Enzalutamide 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 Enzalutamide 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 Enzalutamide. After two days of incubation, reporter activities are assayed.

Cell lines	LNCaP or LNCaP/AR cells
Concentrations	0-10 μM
Incubation Time	1-4 days
Method	Enzalutamide 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 Enzalutamide in media containing 5-10% charcoal-stripped serum.

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

1

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT02012296	Recruiting	Hormone-resistant Prostate Cancer\|Recurrent Prostate Cancer\|Stage IV Prostate Cancer	University of Chicago\|National Cancer Institute (NCI)	2013-12	Phase 1\|Phase 2
NCT01949337	Not yet recruiting	Adenocarcinoma of the Prostate\|Hormone-resistant Prostate Cancer\|Recurrent Prostate Cancer\|Stage IV Prostate Cancer	Alliance for Clinical Trials in Oncology\|National Cancer Institute (NCI)	2013-12	Phase 3
NCT02003924	Recruiting	Nonmetastatic Castration-Resistant Prostate Cancer	Medivation, Inc.\|Astellas Pharma Inc	2013-12	Phase 3
NCT01990196	Not yet recruiting	Prostate Cancer	University of California, Los Angeles	2013-12	Phase 2
NCT02008058	Not yet recruiting	Metastatic Castrate-Resistant Prostate Cancer	UNC Lineberger Comprehensive Cancer Center\|Department of Defense\|Memorial Sloan-Kettering Cancer Center\|Johns Hopkins University\|University of Washington\|Oregon Health and Science University	2013-12

Download Enzalutamide (MDV3100) SDF

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

Solubility (25°C) * <1 mg/ml means slightly soluble or insoluble DMSO 93 mg/mL (200 mM) Water <1 mg/mL (<1 mM) Ethanol <1 mg/mL (<1 mM)
Storage	2 years -20°CPowder
Storage	6 months-80°Cin DMSO

Chemical Name

Stock Solution (1ml DMSO)	1mM	10mM	20mM	30mM
Mass(mg)	0.46444	4.6444	9.2888	13.9332

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Rating

Source

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

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Rating

Source

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

Distinct expression and activity of GSK-3α and GSK-3β in prostate cancer. [Darrington RS, et al. Int J Cancer 2012;131(6):E872-83]
PubMed: 22539113
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
Structural and functional association of androgen receptor with telomeres in prostate cancer cells. [Zhou J, et al. Aging 2013;5(1):3-17]
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
Growth kinetics of CD133-positive prostate cancer cells. [Reyes EE, et al. Prostate 2012;73(7):724-33]
PubMed: 23138940
Constitutively active androgen receptor variants upregulate expression of mesenchymal markers in prostate cancer cells. [Cottard F, et al. PLoS One 2013;8(5):e63466]
PubMed: 23658830
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

Bicalutamide
Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM.
Olaparib (AZD2281, Ku-0059436)
Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM, 300-times less effective against tankyrase-1. Phase 1/2.

Features:A potent PARP inhibitor (currently in late stage clinical trials).
Abiraterone Acetate
Abiraterone Acetate is an acetate salt form of Abiraterone which is a steroidal cytochrome CYP17 inhibitor with IC50 of 72 nM.

Features:Abiraterone is a drug used in castration-resistant prostate cancer.
Abiraterone
Abiraterone is a potent CYP17 inhibitor with IC50 of 2 nM.

Features:Approved for the treatment of docetaxel-treated castration-resistant prostate cancer.
Vemurafenib (PLX4032, RG7204)
Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-Raf^V600E with IC50 of 31 nM.

Features:A novel and potent inhibitor of the B-RAF^V600E oncoprotein.
ARN-509
ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, useful for prostate cancer treatment. Phase 2.

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.

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AZD3514
AZD3514 is a potent and oral androgen receptor downregulator with K_i of 2.2 μM and has ability of reducing AR protein expression.
GW9508
GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner.

Features:The effects of GW9508 on insulin secretion are reversed by GW1100, while linoleic acid-stimulated insulin secretion is partially attenuated by GW1100.
PD123319
PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.
Enzalutamide (MDV3100)
Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.
Bicalutamide
Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM.
MK-2866 (GTx-024)
MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with K_i of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.

Features:The most potent and tissue-selective in vivo activity of SARMs to date, with favorable pharmacokinetic properties.
ARN-509
ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, useful for prostate cancer treatment. Phase 2.
Andarine
Andarine is a selective non-steroidal androgen receptor (AR) agonist with K_i of 4 nM, tissue-selective for anabolic organs.
Galeterone
Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.
Flutamide
Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with K_i values of 55 nM, and primarily used to treat prostate cancer. Phase 4.

Cat.No.	Product Name	Solubility (25°C)
Cat.No.	Product Name	Water	DMSO	Ethanol
S1250	Enzalutamide (MDV3100)	<1 mg/mL	93 mg/mL	<1 mg/mL
S1190	Bicalutamide	<1 mg/mL	86 mg/mL	5 mg/mL
S2840	ARN-509	<1 mg/mL	18 mg/mL	5 mg/mL
S1174	MK-2866 (GTx-024)	<1 mg/mL	78 mg/mL	78 mg/mL
S1908	Flutamide	<1 mg/mL	55 mg/mL	55 mg/mL
S2042	Cyproterone Acetate	<1 mg/mL	83 mg/mL	10 mg/mL
S1140	Andarine	<1 mg/mL	88 mg/mL	88 mg/mL
S2803	Galeterone	<1 mg/mL	24 mg/mL	40 mg/mL
S1304	Megestrol Acetate	<1 mg/mL	33 mg/mL	15 mg/mL
S4054	Spironolactone	<1 mg/mL	83 mg/mL	20 mg/mL
S7040	AZD3514	<1 mg/mL	100 mg/mL	100 mg/mL

Description

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

Androgen-receptor

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). ^[1] Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. ^[2]

Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. ^[1]