MK-0752

• 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].

• 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

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

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 4

• CAS Number :

  [471905-41-6]