ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM and anticancer activity that promotes tumor regression in a xenograft mouse model of breast cancer.
|Solubility (25°C)||DMSO ≥ 60 mg/mL|
|Storage||4°C, dry, sealed|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
 Kazuyuki Kuramoto, et al. Chem Pharm Bull (Tokyo). Novel Indirect AMP-Activated Protein Kinase Activators: Identification of a Second-Generation Clinical Candidate with Improved Physicochemical Properties and Reduced hERG Inhibitory Activity
 Kazuyuki Kuramoto, et al. Bioorg Med Chem. Development of a potent and orally active activator of adenosine monophosphate-activated protein kinase (AMPK), ASP4132, as a clinical candidate for the treatment of human cancer
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