MK-0752 is a potent gamma secretase inhibitor, an enzyme required for Notch pathway activation. MK-0752 reduces Aβ40 production with IC50 of 5 nM in human SH-SY5Y cells. MK-0752 blocks Notch-intracellular domain (ICD) cleavage and its subsequent nuclear translocation in vitro. MK-0752 treatment increases levels of Aβ 1-14, Aβ 1-15 and Aβ 1-16, while decreases levels of Aβ 1-17. Phase I clinical trials has been completed in 2006, and the results reported showed that MK-0752 was well-tolerated in a limited number of patients below 300 mg/m2, and further enrollment was underway to establish the MTD.
Molecular Weight | 442.9 |
Formula | C21H21ClF2O4S |
CAS Number | 471905-41-6 |
Solubility (25°C) | DMSO 79 mg/mL Ethanol 35 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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