| 货号： | ONI-171420 |
| CAS号： | 171179-06-9 |
| 供应商： | 美国 |
| 数量： | 919.0 |
| 英文名： | PD 158780, PD-158780 |
| 保质期： | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
| 保存条件： | 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO |
| 规格： | (5mg/100mg/469mg) |
PD158780 is a very potent inhibitor of EGFR with IC50 of 0.08 nM; pan-specific antagonist of ErbB receptor. IC50 value: 0.08 nM [1] Target: EGFR inhibitor in vitro: PD158780 potently inhibited the LPA-stimulated MAP kinase kinase 1/2 (MKK1/2) activation and EGF receptor tyrosine phosphorylation in HeLa cells, while it had no detectable effect on c-Src kinase activity. PD158780 also inhibited LPA-induced MKK1/2 activation and DNA synthesis in NIH 3T3 cells. Furthermore, we compared LPA-stimulated MKK1/2 and MAP kinase activation, transcriptional activity of the c-fos promoter, and DNA synthesis in B82L cells, which lack endogenous EGF receptor, and B82L cells expressing kinase-defective or wild-type human EGF receptor [2]. in vivo: NRG-1beta dramatically increases gamma oscillation power in hippocampal slices from both rats (2062 +/- 496%) and mice (710 +/- 299%). These effects of NRG-1beta are blocked by PD158780, a pan-specific antagonist of ErbB receptors, and are mediated specifically via ErbB4 receptors, because mice harboring a targeted mutation of ErbB4 do not respond to NRG-1 [3].
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