MK-2866 (GTx-024)

Catalog No.S1174

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.

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MK-2866 (GTx-024) Chemical Structure

MK-2866 (GTx-024) Chemical Structure
Molecular Weight: 389.33

Validation & Quality Control

Quality Control & MSDS

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Product Description

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.
Targets Androgen Receptor [1]
IC50 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]
Features The most potent and tissue-selective in vivo activity of SARMs to date, with favorable pharmacokinetic properties.

Protocol(Only for Reference)

Kinase Assay: [1]

In vitro competitive radioligand binding assay The AR binding affinity of Ostarine is determined using an in vitro competitive radioligand binding assay with [3H]mibolerone (MIB). Briefly, increasing concentrations (0.01-5000 nM) of Ostarine are incubated with rat cytosol, a saturating concentration of [3H]-MIB (1 nM), and 1000 nM triamcinolone acetonide to prevent interaction of MIB with progesterone receptors at 4 °C for 18 hours. At the end of incubation, free and bound [3H]-MIB are separated using the hydroxyapatite method. IC50 value is determined by computer-fitting the data for each ligand by nonlinear regression analysi

Animal Study: [1]

Animal Models Immature castrated male Sprague-Dawley rats
Formulation Dissolved in DMSO, and diluted in saline
Dosages 1 mg/day
Administration Subcutaneous injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Kim J, et al. J Pharmacol Exp Ther, 2005, 315(1), 230-239.

[2] Duke CB, et al. J Med Chem, 2011, 54(11), 3973-3976.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
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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Chemical Information

Download MK-2866 (GTx-024) SDF
Molecular Weight (MW) 389.33
Formula

C19H14F3N3O3

CAS No. 841205-47-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms Enobosarm
Solubility (25°C) * In vitro DMSO 78 mg/mL (200.34 mM)
Ethanol 78 mg/mL (200.34 mM)
Water <1 mg/mL (<1 mM)
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 5 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name (S)-N-(4-cyano-3-(trifluoromethyl)phenyl)-3-(4-cyanophenoxy)-2-hydroxy-2-methylpropanamide

Tech Support

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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