Description
MK-0752 can inhibit gamma secretase with IC50 of 50 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C21H21ClF2O4S
Chemical Name
3-((1r,4s)-4-(4-chlorophenylsulfonyl)-4-(2,5-difluorophenyl)cyclohexyl)propanoic acid
Solubility
DMSO 89 mg/mL Water
In vitro
As a inhibitor of gamma secretase, MK-0752 can inhibit the cleavage of gamma secretase substrates such as amyloid precursor protein and Notch with a concentration that inhibits IC50 of 50 nM. And MK-0752 is developed as a treatment Alzheimers disease. MK-0752 leads to G0-G1 arrest in gamma secretase in T-cell acute lymphatic leukemia cell lines carrying notch-activating mutations with IC 50 of 6.2 nM and has demonstrated activity in neuTtransgenic mouse models of mammary tumors.
In vivo
In animal models of cerebral amyloid formation and deposition, MK-0752 penetrated the brain parenchyma reducing plasmatic amyloid peptide levels by 50% at brain and plasma concentrations of 154 nM and 594 nM. In adults with recurrent solid tumor, the maximum-tolerated dose (MTD) of MK-0752 using the 3-days-on/4-days-off schedule was 450 mg/d with are commended dose of 350mg/d because of fatigue during extended administration.
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