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.
Molecular Weight | 186.17 |
Formula | C10H6N2O2 |
CAS Number | 118409-57-7 |
Solubility (25°C) | DMSO ≥ 25 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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