For research use only.

Catalog No.S2660

16 publications

MK-0752 Chemical Structure

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.

Selleck's MK-0752 has been cited by 16 publications

4 Customer Reviews

  • 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.

  • 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.

  • 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.

  • 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

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Biological Activity

Description MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.
Features A moderately potent γ-secretase inhibitor.
γ secretase(Aβ40) [1] [1]
(in human SH-SY5Y cells)
5 nM
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]

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]


Animal Research:[1]
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  • Animal Models: Cisterna Magna Ported (CMP) Rhesus Monkey Model.
  • Dosages: ≤240 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 89 mg/mL (200.94 mM)
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


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
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% DMSO % % Tween 80 % ddH2O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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

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Frequently Asked Questions

  • Question 1:

    Would you happen to have the half-life information for the drug when used in cell culture?

  • 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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID