MK-0752

Catalog No.S2660

MK-0752 Chemical Structure

Molecular Weight(MW): 442.9

MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.

Size Price Stock Quantity  
In DMSO USD 480 In stock
USD 270 In stock
USD 370 In stock
USD 970 In stock

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1 Customer Review

  • 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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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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.
Targets
γ secretase(Aβ40) [1] [1]
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]

Protocol

Animal Research
+ Expand
  • Animal Models: Cisterna Magna Ported (CMP) Rhesus Monkey Model.
  • Formulation: MK-0752 is dissolved in water.
  • 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 <1 mg/mL
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 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 Information

Molecular Weight 442.9
Formula

C21H21ClF2O4S

CAS No. 471905-41-6
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01295632 Completed Advanced Cancer Merck Sharp & Dohme Corp. February 2011 Phase 1
NCT01243762 Terminated Neoplasms Malignant Merck Sharp & Dohme Corp. November 2010 Phase 1
NCT01098344 Completed Pancreatic Cancer Cancer Research UK April 2010 Phase 1
NCT00803894 Completed Healthy Merck Sharp & Dohme Corp. December 2008 Phase 1
NCT00572182 Terminated Brain and Central Nervous System Tumors Pediatric Brain Tumor Consortium|National Cancer Institute (NCI) July 2008 Phase 1
NCT00756717 Active, not recruiting Breast Cancer Loyola University|Merck Sharp & Dohme Corp. May 2008 --

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

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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