BIBX 1382 is a new selective EGFR kinase inhibitor that do not block the activity of other tyrosine kinases.Tumor growth inhibition by BIBX1382 coincided with reduced pEGFR and Ki-67 levels in vivo, which is in accordance with the expected effect of EGFR inhibitors.BIBX1382 was an epidermal growth factor receptor inhibitor under clinical investigation for treatment of cancer.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥50 mg/mL;Water ≥50 mg/mL|
Cynomolgus monkey as a surrogate for human aldehyde oxidase metabolism of the EGFR inhibitor BIBX1382.
Hutzler JM, et al. Drug Metab Dispos. 2014 Oct;42(10):1751-60. PMID: 25035284.
Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives.
Solca FF, et al. J Pharmacol Exp Ther. 2004 Nov;311(2):502-9. PMID: 15199094.
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