IMR-1 is a cell penetrant and potent inhibitor of Notch transcriptional activation complex that disrupted the recruitment of Mastermind-like 1 (Maml1) to the Notch transcriptional activation complex on chromatin. IMR-1 potently inhibits the growth of Notch-dependent cancer cell lines, and inhibits growth of patient-derived tumor xenografts. IMR-1 is hydrolyzed in vivo to acid metabolite IMR-1A.
|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.
|Solubility||DMSO: 20 mg/mL
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