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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 |
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AZD8931 (Sapitinib) is an equipotent, reversible inhibitor of Signaling by EGFR, ERBB2 (HER2), and ERBB3 with IC50 of 4, 3, 4 nM respectively. |
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