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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Endocrinology & Hormones>Androgen Receptor Antagonists>Enzalutamide
Enzalutamide
  • Enzalutamide

Enzalutamide NEW

Price $40 $51 $68
Package 5mg 10mg 25mg
Min. Order:
Supply Ability: 10g
Update Time: 2024-11-19

Product Details

Product Name: Enzalutamide CAS No.: 915087-33-1
Purity: 99.67% Supply Ability: 10g
Release date: 2024/11/19

Product Introduction

Bioactivity

NameEnzalutamide
DescriptionEnzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP) that activates autophagy, exhibits antitumor activity, and is commonly used in treating desmoplasia-resistant prostate cancer.
Cell ResearchFor in vitro experiments, LNCaP or LNCaP/AR cells (10^4 cells/well) were androgen-starved by growth in media containing 5-10% charcoal-stripped serum for 3-5 days. Then the cells were challenged with various concentrations of R1881, bicalutamide, RD162 or MDV3100 in media containing 5-10% charcoal-stripped serum [1].
Animal ResearchIn vivo tumorigenicity experiments were done by subcutaneous injection of 10^6 cells (100 uL in 50% Matrigel and 50% growth media) into the flanks of castrated male SCID mice. Daily gavage treatment (using a formulation of 1% carboxymethyl cellulose, 0.1% Tween-80, 5% DMSO) was initiated when tumor size reached ~100 mm3. Tumor size was measured weekly in three dimensions (l x w x d) with calipers. For in vivo luciferase imaging, d-luciferin substrate (100 μL, 15 mg/mL) was injected intraperitoneally. After 5 minutes, mice were anesthetized using isofluorane and imaged using a cooled charged-coupled device IVIS camera. Data were analyzed using Living Image 2.30 software [1].
In vitroMETHODS: Human prostate cancer cells LNCaP, PC3 and human osteosarcoma cells SJSA-1 were treated with Enzalutamide (0.01-100 μM) for 1 h. Cell viability was measured using MTT. RESULTS: Enzalutamide was shown to decrease the viability of all cell lines, with LD50s of 12 μM, 23.4 μM, and 34.7 μM for LNCaP, PC3, and SJSA-1 cell lines, respectively. [1] METHODS: Human prostate cancer cells VCaP were treated with Enzalutamide (10 μM) for 1-3 days, and the expression levels of target proteins were detected by Western Blot. RESULTS: Enzalutamide up-regulated cleaved-PARP expression and induced apoptosis in human prostate cancer cells. [2]
In vivoMETHODS: To assay antitumor activity in vivo, Enzalutamide (1-50 mg/kg) was administered by gavage once daily for twenty-eight days to CB17SCID mice bearing human desmoplastic resistance tumor (CRPC) LNCaP-AR-Lux. RESULTS: Enzalutamide induced regression of tumor volume in a CRPC xenograft model and apoptosis in AR overexpanded prostate cancer cells. [3] METHODS: To assess the role of AR in bone metabolism and bone growth after sexual maturation, Enzalutamide (10-100 mg/kg, 1% carboxymethyl cellulose+0.5% Tween 80+5% dimethylsulfoxide) was administered orally to C57BL/6N mice once daily for twenty-one days. RESULTS: Enzalutamide decreased the amount of bone in the axial skeleton, and Enzalutamide significantly reduced the mechanical strength of the axial skeleton. After sexual maturity, Enzalutamide reduced bone mass in the axial skeleton but not in the appendicular skeleton of male mice. [4]
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility InformationEthanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 60 mg/mL (129.19 mM)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 8.5 mg/mL (18.3 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
KeywordsLNCaP | prostate | Androgen Receptor | cell | Inhibitor | Autophagy | MDV-3100 | MDV 3100 | inhibit | Enzalutamide
Inhibitors RelatedStavudine | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Taurine | Curcumin | Oxyresveratrol | Paeonol | Naringin | Gefitinib
Related Compound LibrariesBioactive Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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