MK-0752

Catalog No.S2660

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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MK-0752 Chemical Structure

MK-0752 Chemical Structure
Molecular Weight: 442.9

Validation & Quality Control

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Quality Control & MSDS

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Product Information

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Product Description

Biological Activity

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

Protocol(Only for Reference)

Animal Study: [1]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Cook JJ, et al. J Neurosci, 2010, 30(19), 6743-6750.

[2] Harrison H, et al. Cancer Res, 2010, 70(2), 709-718.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

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 Institut  ...more Pediatric Brain Tumor Consortium|National Cancer Institute (NCI) July 2008 Phase 1

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Chemical Information

Download MK-0752 SDF
Molecular Weight (MW) 442.9
Formula

C21H21ClF2O4S

CAS No. 471905-41-6
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 89 mg/mL (200.94 mM)
Ethanol 45 mg/mL (101.6 mM)
Water <1 mg/mL (<1 mM)
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 Name 3-((1r,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid

Customer Product Validation(1)


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Rating
Source Oncotarget 2014 5(2), 363-74. MK-0752 purchased from Selleck
Method Cell viability assays
Cell Lines Hs683-Rl glioblastoma cells
Concentrations
Incubation Time
Results Subsequently, it assessed the inhibitory effects of the clinically available GSIs RO4929097, BMS-708163, LY450139, and MK-0752 on the Notch pathway by determining HES1 expression after GSI treatment.

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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