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MK-0752 γ-secretase inhibitor

Catalog No.A4006
Size Price Stock Qty
10mM (in 1mL DMSO)
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Evaluation Sample
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Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Chen X, Gong L, et al. "Sequential combination therapy of ovarian cancer with cisplatin and γ-secretase inhibitor MK-0752." Gynecol Oncol. 2016 Mar;140(3):537-44. PMID:26704638

Quality Control

Chemical structure


Related Biological Data


Related Biological Data


Related Biological Data


Biological Activity

Targets γ-secretase          
IC50 5 nM          


Cell experiment: [1]

Cell lines

SH-SY5Y cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

IC50: 5 nM.


As a moderately potent γ-secretase inhibitor, MK-0752 inhibited the production of Aβ40 in a dose-dependent manner with an IC50 of 5 nM in human SH-SY5Y cells.

Animal experiment : [1]

Animal models

Male CMP rhesus monkeys

Dosage form

Oral administration, 60 mg/kg and 240mg/kg


Oral administration of MK-0752 demonstrated a dose-related reduction of Aβ levels. After 48 h, the Aβ levels with 240mg/kg treatment only recovered to 50%of baseline, while the 60mg/kg treatment group reached baseline at 30 h without overshoot. Plasma Aβ levels rebounded above baseline after MK-0752 inhibition (60 mg/kg, h 33–48).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.


[1] Cook J J, Wildsmith K R, Gilberto D B, et al. Acute γ-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-β production to alternative APP fragments without amyloid-β rebound[J]. The Journal of Neuroscience, 2010, 30(19): 6743-6750.

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Chemical Properties

Cas No. 471905-41-6 SDF Download SDF
Synonyms MK 0752, MK0752
Chemical Name 3-[4-(4-chlorophenyl)sulfonyl-4-(2,5-difluorophenyl)cyclohexyl]propanoic acid
Canonical SMILES C1CC(CCC1CCC(=O)O)(C2=C(C=CC(=C2)F)F)S(=O)(=O)C3=CC=C(C=C3)Cl
Formula C21H21ClF2O4S M.Wt 442.9
Solubility >22.2mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Research Update

1. Phase I pharmacologic and pharmacodynamic study of the gamma secretase (Notch) inhibitor MK-0752 in adult patients with advanced solid tumors. J Clin Oncol. 2012 Jul 1;30(19):2307-13. doi: 10.1200/JCO.2011.39.1540. Epub 2012 Apr 30.
MK-0752, an inhibitor of γ-secretase, has been assessed for safety, maximum-tolerated dose, PKs, pharmacodynamics and antitumor efficacy in a phase I study.
2. Phase I trial of MK-0752 in children with refractory CNS malignancies: a pediatric brain tumor consortium study. J Clin Oncol. 2011 Sep 10;29(26):3529-34. doi: 10.1200/JCO.2011.35.7806. Epub 2011 Aug 8.
The MTD, DLTs and pharmacokinetic properties of MK-0752, a γ-secretase inhibitor, have been evaluated in children with refractory or recurrent CNS malignancies.
4. Determination of the gamma-secretase inhibitor MK-0752 in human plasma by online extraction and electrospray tandem mass spectrometry (HTLC-ESI-MS/MS). J Chromatogr B Analyt Technol Biomed Life Sci. 2010 Sep 1;878(25):2348-52. doi: 10.1016/j.jchromb.2010.07.019. Epub 2010 Jul 30.
The concentration of MK-0752, a γ-secretase inhibitor, in human plasma can be determined by the HTLC-ESI-MS/MS method, which was used to measure plasma MK-0752 levels in a Phase I study of pediatric patients with recurrent or refractory brain tumors.


MK-0752 is a potent gamma secretase inhibitor in clinical development (IC50 ~50 nM). Gamma secretase is an important component in the NOTCH cleavage machinery that catalyzes the cleavage of receptor protein substrates within their transmembrane domain. Inhibition of Notch inhibits BC cell proliferation in vitro. Notch signaling requires gamma secretase, which cleaves Notch, releasing the Notch intracellular domain (NICD) to activate transcription of target genes. NOTCH signaling plays an important role in normal tissue development, cell fate determination, proliferation, and survival. NOTCH signaling is activated following the binding of cognate ligands that include Delta1, Delta2, and Delta3 and Jagged1 and Jagged2.


I. E. Krop, M. Kosh, I. Fearen, J. Savoie, A. Dallob, C. Matthews, J. Stone, E. Winer, S. J. Freedman and P. Lorusso. Phase I pharmacokinetic (PK), and pharmacodynamic (PD) trial of the novel oral Notch inhibitor MK-0752 in patients (pts) with advanced breast cancer (BC) and other solid tumors. J Clin Oncol (Meeting Abstracts) June 2006 vol. 24 no. 18_suppl 10574.

Maryam Fouladi, Clinton F. Stewart, James Olson, Lars M. Wagner, Arzu Onar-Thomas, Mehmet Kocak, Roger J. Packer, Stewart Goldman, Sridharan Gururangan, Amar Gajjar, Tim Demuth, Larry E. Kun, James M. Boyett and Richard J. Gilbertson. Phase I Trial of MK-0752 in Children With Refractory CNS Malignancies: A Pediatric Brain Tumor Consortium Study. JCO September 10, 2011 vol. 29 no. 26 3529-3534