Other grades of this product :
| PD 166866 Basic information |
| PD 166866 Chemical Properties |
| Melting point | 291-293°C | | storage temp. | 2-8°C | | solubility | DMSO: ≥10mg/mL | | form | Off-white solid | | color | off-white to light tan |
| Hazard Codes | Xn | | Risk Statements | 22 | | WGK Germany | 1 |
| PD 166866 Usage And Synthesis |
| Description | PD 166866 is a potent inhibitor of fibroblast growth factor receptor 1 (FGFR1; IC50 = 52.4 nM; Ki = 45.2 nM). It is selective for FGFR1 over PDGFR, EGFR, C-SRC, MEK, PKC, insulin receptor tyrosine kinase, and CDK4 (IC50s = >50 μM). PD 166866 inhibits FGFR1 autophosphorylation in NIH3T3 and L6 cells (IC50s = 10.8 and 3.1 nM, respectively) and inhibits phosphorylation of MAPK (IC50s = 4.3 and 7.9 nM for the 44- and 42-kDa MAPK isoforms, respectively). It reduces FGF- but not EGF- or PDGF-stimulated growth of L6 cells and inhibits microvessel outgrowth from human placental arteries in vitro. PD 166866 inhibits the growth of non-small cell lung cancer (NSCLC) cell lines in a dose-dependent manner and reduces migration of VL-8 cells at a concentration of 10 μM. | | Chemical Properties | Off-White Solid | | Uses | A novel potent ATP competitive pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. An inhibitor of the basic fibroplast growth factor (bFGF). | | Biochem/physiol Actions | PD-166866 is a selective inhibitor of the FGF-1 receptor tyrosine kinase (FGFR1) with IC50 = 55 nM, and no effect on c-Src, PDGFR-b, EGFR or insulin receptor tyrosine kinases or MEK, PKC, and CDK4. |
| PD 166866 Preparation Products And Raw materials |
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