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PD168393 is an irreversible EGFR inhibitor with IC50 of 0.70 nM, irreversibly alkylate Cys-773; inactive against insulin, PDGFR, FGFR and PKC. PD168393 inhibits heregulin-induced tyrosine phosphorylation in MDA-MB-453 cells with IC50 of 5.7 nM. PD168393 is inactive against insulin, PDGF and basic FGFR TKs as well as PKC. PD168393 inhibits EGF-mediated tyrosine phosphorylation in HS-27 human fibroblasts with IC50 of 1-6 nM but has little effect on FGF- or PDGF-mediated tyrosine phosphorylation. PD 168393 produces tumor growth inhibition of 115% in A431 human epidermoid carcinoma xenograft in nude mice, with 50% reduced phosphotyrosine content of EGFR. PD 168393 also shows a low plasma concentration.
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Source | Neuro Oncol (2012). Figure 1. PD168393 |
| Method | apoptosis assay | |
| Cell Lines | MPNST cells | |
| Concentrations | 2 μM | |
| Incubation Time | 24–48 h | |
| Results | Taken together, these data indicate that PD168393-induced block in erbB signaling is largely cytostatic and has no effect on MPNST cell apoptosis. |
| Molecular Weight | 369.22 |
| Formula | C17H13BrN4O |
| CAS Number | 194423-15-9 |
| Solubility (25°C) | DMSO 34 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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