MK-2866 (GTx-024)

Catalog No.S1174 Synonyms: Enobosarm, ostarine

MK-2866 (GTx-024) Chemical Structure

Molecular Weight(MW): 389.33

MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.

Size Price Stock Quantity  
In DMSO USD 260 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock
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Biological Activity

Description MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with Ki 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.
Targets
Androgen Receptor [1]
3.8 nM(Ki)
In vitro

Ostarine at the concentration of 10 nM modulates the transcriptional activity of AR in CV-1 cells cotransfected with a human AR expression vector, a luciferase reporter vector, and a control β-galactosidase vector, with 94%-100% relative activity of the transcriptional activation observed for 1 nM DHT. [1] [2]

In vivo After intravenous administration of Ostarine at a single dose of 10 mg/kg, plasma concentration of Ostarine declines slowly, exhibiting a longer terminal half-life of 6.0 hours, as compared to that of other related cyano/nitro group-substituted SARMs with terminal halflives of 2.6-4.0 hours. Ostarine exhibits significantly androgenic and anabolic activity by stimulating the growth of prostate, seminal vesicles, and levator ani muscle when administered in castrated male rats; Ostarine is more potent than other cyano/nitro group-substituted SARMs. Ostarine restores the weight of the prostate to 39.2%, and seminal vesicle 78.8%, and stimulates the growth of levator ani muscle to a greater extent of 141.9% as compared with that of androgenic organs. Ostarine exhibits the highest in vivo androgenic and anabolic activity of any AR nonsteroidal agonist examined to date, with ED50 values of 0.12, 0.39 and 0.03 mg/day in prostate, seminal vesicles, and levator ani muscle, respectively, being 4 times as potent as testosterone propionate (TP) in levator ani muscle. At low dose of 0.03 mg/day, Ostarine is sufficient to exert efficacious and selective activity in anabolic tissues. [1]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Immature castrated male Sprague-Dawley rats
  • Formulation: Dissolved in DMSO, and diluted in saline
  • Dosages: 1 mg/day
  • Administration: Subcutaneous injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (200.34 mM)
Ethanol 78 mg/mL (200.34 mM)
Water slightly soluble or insoluble
In vivo Add solvents individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 389.33
Formula

C19H14F3N3O3

CAS No. 841205-47-8
Storage powder
in solvent
Synonyms Enobosarm, ostarine

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02971761 Not yet recruiting Androgen Receptor Positive|Estrogen Receptor Negative|HER2/Neu Negative|Progesterone Receptor Negative|Recurrent Breast Carcinoma|Stage III Breast Cancer|Stage IIIA Breast Cancer|Stage IIIB Breast Cancer|Stage IIIC Breast Cancer|Stage IV Breast Cancer|Triple-Negative Breast Carcinoma City of Hope Medical Center|National Cancer Institute (NCI) January 2017 Phase 2
NCT02746328 Not yet recruiting ER+ and AR+ Breast Cancer GTx|Martin Performance April 2016 Phase 2
NCT02658448 Recruiting Stress Urinary Incontinence GTx January 2016 Phase 2
NCT02463032 Recruiting ER+ and AR+ Breast Cancer GTx August 2015 Phase 2
NCT02368691 Recruiting Triple Negative Breast Cancer GTx June 2015 Phase 2
NCT01616758 Active, not recruiting Metastatic Breast Cancer GTx April 2013 Phase 2

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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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Androgen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID