GDC-0973 is a potent and selective mitogen-activated protein (MAP)/extracellular signal-regulated kinase (ERK) kinase (MEK) inhibitor. GDC-0973 is known as mitogen activated protein kinase kinase (MAPKK). GDC-0973 is a key component of the RAS/RAF/MEK/ERK pathway, which is frequently activated in human tumors.
|Cell lines||Human 888MEL (BRAFV600E) mutant melanoma cell lines|
|Preparation method||Plating cells in quadruplicate at a density of 3,000 per well in 384-well plates in normal growth medium and allowing to adhere overnight. Adding compounds in 10 concentrations based on a 3-fold dilution series. Using the CellTiter-Glo Luminescent Cell Viability Assay to measure cell viability 72 h later.|
|Incubation time||4 days|
|Animal models||Human A375.X1 BRAFV600E mutant melanoma xenograft|
|Administration||orally daily (QD) for 2 1 consecutive days|
|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.
Bridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor.
Wong H, et al. Clin Cancer Res. 2012 Jun 1;18(11):3090-9. PMID: 22496205.
|Related MEK Products|
BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively.
LY2801653 is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).
Refametinib (BAY 86-9766, RDEA119) is a potent, highly selective and ATP non-competitive inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.
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