MK-0752

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

MK-0752 Chemical Structure

MK-0752 Chemical Structure

CAS: 471905-41-6

Selleck's MK-0752 has been cited by 22 Publications

4 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.21%
99.21

MK-0752 Related Products

Choose Selective 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.
Features A moderately potent γ-secretase inhibitor.
Targets
[1]
(in human SH-SY5Y cells)
5 nM
In vitro
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
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 Animal Models Cisterna Magna Ported (CMP) Rhesus Monkey Model.
Dosages ≤240 mg/kg
Administration Administered via p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01295632 Completed
Advanced Cancer
Merck Sharp & Dohme LLC
February 2011 Phase 1
NCT00572182 Terminated
Brain and Central Nervous System Tumors
Pediatric Brain Tumor Consortium|National Cancer Institute (NCI)
July 2008 Phase 1

Chemical Information & Solubility

Molecular Weight 442.9 Formula

C21H21ClF2O4S

CAS No. 471905-41-6 SDF Download MK-0752 SDF
Smiles C1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 89 mg/mL ( (200.94 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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.

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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