AMG-47a displays subnanomolar inhibition against Lck, and low (<10 nM) inhibition against other hard to inhibit kinases such as KDR and SRC and MAPK α (p38α). In addition, at slightly higher doses but well under 10 μM, AMG-47a effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2 μM. AMG-47a selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells.
|Cell lines||HeLa cells|
|Preparation method||Cells were treated with varying concentrations of AMG-47a, Ponatinib, and Torin-1. Media and compound were refreshed after 3 days on cells being treated for 5 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.
|Solubility||34 mg/mL in DMSO|
A high-throughput assay for small molecule destabilizers of the KRAS oncoprotein.
Carver J, et al. PLoS One. 2014 Aug 5;9(8):e103836. PMID: 25093678.
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