MK-0752

• UNSPSC Description:

  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].

• Target Antigen:

  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 Weight:

  442.90

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  Phase 4

• CAS Number:

  471905-41-6