MK-0752

MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo[1][2].

Product Specifications

CAS Number

[471905-41-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

γ-secretase

Type

Reference compound

Related Pathways

Neuronal Signaling; Stem Cell/Wnt

Applications

Cancer-programmed cell death

Field of Research

Neurological Disease; Cancer

Assay Protocol

https://www.medchemexpress.com/MK-0752.html

Purity

99.35

Solubility

DMSO : ≥ 100 mg/mL|Ethanol : 10 mg/mL (ultrasonic)

Smiles

O=S([C@@]1(C2=C(C=CC(F)=C2)F)CC[C@@H](CCC(O)=O)CC1)(C3=CC=C(Cl)C=C3)=O

Molecular Formula

C21H21ClF2O4S

Molecular Weight

442.90

Precautions

H302, H315, H319, H335

References & Citations

[1]Cook JJ, et al. Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound. J Neurosci. 2010;30 (19) :6743-6750.|[2]Krop I, et al. 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;30 (19) :2307-2313.