MK-0752
For research use only.
Catalog No.S2660
16 publications
CAS No. 471905-41-6
MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.
4 Customer Reviews
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HES1 expression after treatment with clinically available GSIs R04929097, BMS-708163, LY450139, and MK-0752 as determined by qRT-PCR.
Oncotarget 2014 5(2), 363-74. MK-0752 purchased from Selleck.
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Spontaneous migration in the “wound-healing assay.” Representative images of wound closure 16 hours after the scratch. Original magnification: ×200. Bar graphs represent migrated cells/field expressed as mean ± S.D.
Neoplasia, 2018, 21(1):93-105. MK-0752 purchased from Selleck.
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Western blot for Notch receptors in B5725 and C0321 cells treated with 6 μM of MK-0752 for 24 h. Control was incubation with DMSO.
Cancer Biol Ther, 2014, 15(5):633-42. MK-0752 purchased from Selleck.
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Jurkat cells were treated with (D) TRAIL (20 ng/ml), MK-0752 (50 µM) or a combination of the two for 48 h. Vehicle control for (D), 0.1% (v/v) dimethyl sulfoxide. Data shown are the mean ± standard error of the mean of ≥3 independent experiments. *P≤0.05, **P≤0.01. TRAIL, tumour necrosis factor-related apoptosis-inducing ligand.
Oncol Lett, 2016, 12(4):2900-2905. MK-0752 purchased from Selleck.
Purity & Quality Control
Choose Selective Gamma-secretase Inhibitors
Biological Activity
| Description | MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2. | ||||
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| Features | A moderately potent γ-secretase inhibitor. | ||||
| Targets |
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| In vitro |
MK-0752 is identified as a moderately potent γ-secretase inhibitor, which reduces Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells. [1] In vitro, MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation. [2] |
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| In vivo | MK-0752 (240 mg/kg) reduces the generation of newly produced Aβ with 90% decrease of AUV in the brain of rhesus monkeys. In addition, MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15, and Aβ 1-16 , while decreases levels of Aβ 1-17. [1] In guinea-pigs, oral administration of MK-0752 (10 mg/kg -30 mg/kg) results in the dose-dependent reduction of Aβ40 in plasma, brain and cerebrospinal fluid (CSF) with IC50 of 440 nM in brain. [2] |
Protocol
| Animal Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 89 mg/mL (200.94 mM) |
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| Ethanol | 45 mg/mL (101.6 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% propylene glycol, 5% Tween 80, 65% D5W For best results, use promptly after mixing. |
30 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 | 442.9 |
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| Formula | C21H21ClF2O4S |
| CAS No. | 471905-41-6 |
| Storage |
powder in solvent |
| Synonyms | N/A |
| Smiles | C1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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| NCT01295632 | Completed | Drug: ridaforolimus|Drug: MK-0752|Drug: MK-2206 | Advanced Cancer | Merck Sharp & Dohme Corp. | February 2011 | Phase 1 |
| NCT00572182 | Terminated | Drug: MK-0752 | Brain and Central Nervous System Tumors | Pediatric Brain Tumor Consortium|National Cancer Institute (NCI) | July 2008 | Phase 1 |
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
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Question 1:
Would you happen to have the half-life information for the drug when used in cell culture?
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Answer:
The half life of S2660 in patients is about 15 hours. But its half-life time in different cell culture might be various and we generally recommend replenishing with fresh drug every 24-48 hours.
