GDC-0994 potently inhibits phospho-p90RSK in tumor cells. GDC-0994 inhibits both ERK phosphorylation and activation of ERK-mediated signal transduction pathways. GDC-0994 subsequently prevents ERK-dependent tumor cell proliferation and survival.
|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.
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VX-11e is a potent, selective, and orally bioavailable ERK2 inhibitor with Ki of <2 nM, over 200-fold selective over other kinases tested.
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