Buy Enzalutamide (MDV3100) | Androgen Receptor Chemicals | Price | IC50

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Product Citations(8)

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

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

Aging, 2013, ahead of print

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

Mol Cell Endocrinol, 2013, 365(1), 95-107
Prostate, 2012, ahead of print

PLoS One, 2013, 8(5):e63466

PLoS One, 2012, 8(1), e53701

Customer Reviews(2) in vivo invitation

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

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

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

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

Product Description

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

Biological Activity

Description	Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.
Targets	Androgen-receptor
IC50	36 nM ^[1]
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]
If your cell culture is contaminated by mycoplasma, please use our new product MycoClean™ Mycoplasma Removal Kit (Catalog No. K9000). This is a novel, efficient and safe kit to remove mycoplasma.
In vivo	Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. ^[1]
Features

Protocol(Only for Reference)

Kinase Assay: ^[3]

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 Assay: ^[1]

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 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

1

References

Chemical Information

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 Water <1 mg/mL Ethanol <1 mg/mL
Storage	2 years -20°CPowder
Storage	6 months-80°Cin DMSO

Chemical Name

Preparing Stock Solutions

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

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Customer Reviews (2)

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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.

Product Citations (8)

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
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;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
Growth kinetics of CD133-positive prostate cancer cells. [Reyes EE, et al. Prostate 2012;ahead of print]
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

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

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AZD3514
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Enzalutamide (MDV3100)

Validation & Quality Control Free Sample Request

Product Citations(8)

Customer Reviews(2) in vivo invitation

Quality Control & MSDS

Related Compound Libraries

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

Product Information

Compare Androgen Receptor Chemicals

Research Area

Product Description

Biological Activity

Protocol(Only for Reference)

Kinase Assay: ^[3]

Cell Assay: ^[1]

Animal Study: ^[1]

References

Chemical Information

Preparing Stock Solutions

Research Area

Customer Reviews (2)

Product Citations (8)

Tech Support & FAQs

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

Related Androgen Receptor Chemicals

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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

Choose Your Country or Region

Product Categories

Enzalutamide (MDV3100)

Validation & Quality Control Free Sample Request

Product Citations(8)

Customer Reviews(2) in vivo invitation

Quality Control & MSDS

Related Compound Libraries

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

Product Information

Compare Androgen Receptor Chemicals

Research Area

Product Description

Biological Activity

Protocol(Only for Reference)

Kinase Assay: [3]

Cell Assay: [1]

Animal Study: [1]

References

Chemical Information

Preparing Stock Solutions

Research Area

Customer Reviews (2)

Product Citations (8)

Tech Support & FAQs

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

Related Androgen Receptor Chemicals

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Kinase Assay: ^[3]

Cell Assay: ^[1]

Animal Study: ^[1]