AG 18 (Tyrphostin 23) is an inhibitor of epidermal growth factor receptor (EGFR) and platelet-derived growth factor receptor (PDGFR) kinase with IC50 values of 35 and 25 μM respectively. AG 18 inhibits EGF-stimulated cell proliferation. AG 18 also acts as a mitochondrial uncoupler that alters phosphorylation-dependent cell signaling. AG18 increased the rate of oxygen consumption and reduced cellular ATP by approximately 90% in the absence of the muscarinic agonist carbachol. AG 18 (10 μM) decreases the potency of 5-HT 4-fold and reduces the maximal contraction to 5-HT in the carotid artery. AG18 blocked parotid phosphorylation events only at concentrations that reduced ATP content. AG18 (RG-50810) also activated AMPK and/or uncoupled mitochondria in PC12, HeLa, and HEK293 cells.
|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 ≥ 25 mg/mL|
Evidence that tyrphostins AG10 and AG18 are mitochondrial uncouplers that alter phosphorylation-dependent cell signaling.
Soltoff SP. J Biol Chem. 2004 Mar 19;279(12):10910-8. PMID: 14688271.
Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.
Gazit A, et al. J Med Chem. 1989 Oct;32(10):2344-52. PMID: 2552117.
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