Name | PD-166866 (PD166866) |
Synonyms | CS-2496 PD 166866 PD-166866 PD-166866 (PD166866) FGF Receptor Tyrosine Kinase Inhibitor tert-butyl (2-amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl)carbamate 1-(2-aMino-6-(3,5-diMethoxyphenyl)pyrido[2,3-d]pyriMidin-7-yl)-3-(tert-butyl)urea N-[2-AMino-6-(3,5-diMethoxyphenyl)pyrido[2,3-d]pyriMidin-7-yl]-N'-(1,1-diMethylethyl) |
CAS | 192705-79-6 |
Molecular Formula | C20H24N6O3 |
Molar Mass | 396.44 |
Melting Point | 291-293°C |
Solubility | DMSO: ≥10mg/mL |
Appearance | Off-white solid |
Color | off-white to light tan |
Storage Condition | 2-8°C |
In vitro study | PS166866 can cause mitochondrial defects and oxidative stress. PD 166866 inhibits human full-length FGFR-1 tyrosine kinase with IC50 of 52.4±0.1 nM, but at concentrations as high as 50 μm, it inhibits c-Src, PDGFR-β, EGFR or insulin receptor tyrosine kinase, MPK, PKC and CDK4 had no effect. PD166866 is a potent inhibitor of bFGF-mediated receptor autophosphorylation in NIH 3T3 cells expressing endogenous FGFR-1 and L6 cells overexpressing human FGFR-1 tyrosine kinase. In vascular smooth muscle cells, A432 or NIHIR cells, PD166866 had no inhibitory effect on PDGF, EGF or insulin-stimulated receptor autophosphorylation, indicating a high selectivity of FGFR-1. In addition, PD166866 inhibits microvascular growth (angiogenesis) in cultured human placental artery fragments. In L6 cells, 42-and 44-kDa MAPK were inhibited with an IC50 of 7.9 nM and 4.3 nM, respectively. PD166866 can inhibit autophagy by inhibiting Akt/mTOR signaling pathway. |
Hazard Symbols | Xn - Harmful |
Risk Codes | 22 - Harmful if swallowed |
WGK Germany | 1 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.522 ml | 12.612 ml | 25.224 ml |
5 mM | 0.504 ml | 2.522 ml | 5.045 ml |
10 mM | 0.252 ml | 1.261 ml | 2.522 ml |
5 mM | 0.05 ml | 0.252 ml | 0.504 ml |
biological activity | PD-166866 is a synthetic small molecule that inhibits the tyrosine kinase activity of FGFR1, it is highly selective for FGFR1 and inhibits the self-phosphorylation activity of FGFR1. |
Target | TargetValue FGFR1 (Cell-free assay) 52.4 nM |
Target | Value |
FGFR1 (Cell-free assay) | 52.4 nM |
In vitro studies | PS166866 can cause mitochondrial defects and oxidative stress. PD 166866 inhibits human full-length FGFR-1 tyrosine kinase with IC50 of 52.4±0.1 nM, but at concentrations as high as 50 μm, it inhibits c-Src, PDGFR-β, EGFR or insulin receptor tyrosine kinase, MPK, PKC and CDK4 had no effect. PD166866 is a potent inhibitor of bFGF-mediated receptor autophosphorylation in NIH 3T3 cells expressing endogenous FGFR-1 and L6 cells overexpressing human FGFR-1 tyrosine kinase. In vascular smooth muscle cells, A432 or NIHIR cells, PD166866 had no inhibitory effect on PDGF, EGF or insulin-stimulated receptor autophosphorylation, indicating a high selectivity of FGFR-1. In addition, PD166866 inhibits microvascular growth (angiogenesis) in cultured human placental artery fragments. In L6 cells, 42-and 44-kDa MAPK were inhibited with an IC50 of 7.9 nM and 4.3 nM, respectively. PD166866 can inhibit autophagy by inhibiting Akt/mTOR signaling pathway. |