ARRY-380 is an orally bioavailable, potent, selective, small-molecule tyrosine kinase HER2 and p95-HER2 inhibitor with an IC50 of 8 and 7 nM, respectively. However, ARRY-380 inhibits EGFR with an IC50 of 4 μM. ARRY-380 is about 500-fold selective for HER2 versus EGFR. ARRY-380 produces significantly antitumor activities in multiple HER2-dependent tumor xenograft models and generates additive activity in combination with standard-of-care agents. ARRY-380 is in a phase I clinical trial for the treatment of breast 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 100 mg/mL|
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