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MK-0752

Name: MK-0752
Brand: Selleck Chemicals
SKU: S2660
Rating: 5 (19 reviews)

Catalog No.S2660

For research use only.

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

CAS No. 471905-41-6

Selleck's MK-0752 has been cited by 19 publications

Purity & Quality Control

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Gamma-secretase Signaling Pathway Map

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]	Aβ ^[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]

Protocol (from reference)

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

References

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. Click to purchase: Tween 80	30 mg/mL

Chemical Information

Molecular Weight	442.9
Formula	C₂₁H₂₁ClF₂O₄S
CAS No.	471905-41-6
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl

Download MK-0752 SDF

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:μL Number of animals:

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

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.

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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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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