All AbMole products are for research use only, cannot be used for human consumption.
.gif)
In vitro: The treatment with PD166866 apparently causes a mitochondrial deficit and an oxidative stress. PD 166866 inhibits human full-length FGFR-1 tyrosine kinase with an IC50 value of 52.4 ± 0.1 nM but has no effect on c-Src, platelet-derived growth factor receptor-β, epidermal growth factor receptor or insulin receptor tyrosine kinases or on mitogen-activated protein kinase, protein kinase C and CDK4 at concentrations as high as 50 μM. PD 166866 is a potent inhibitor of basic fibroblast growth factor (bFGF)-mediated receptor autophosphorylation in NIH 3T3 cells expressing endogenous FGFR-1 and in L6 cells overexpressing the human FGFR-1 tyrosine kinase, confirming a tyrosine kinase-mediated mechanism. PD 166866 does not inhibit platelet-derived growth factor, epidermal growth factor or insulin-stimulated receptor autophosphorylation in vascular smooth muscle, A431 or NIHIR cells, respectively, further supporting its specificity for the FGFR-1. Besides, PD 166866 is found to be a potent inhibitor of microvessel outgrowth (angiogenesis) from cultured artery fragments of human placenta. Phosphorylated 44- and 42-kDa MAPK isoforms are inhibited in L6 cells by PD 166866 with IC50 values of 4.3 and 7.9 nM, respectively. PD166866 induces autophagy through repressing Akt/mTOR signaling pathway.
| Cell Experiment | |
|---|---|
| Cell lines | HeLa cells |
| Preparation method | HeLa cells are treated with PD166866 for 24 hours, the growth medium is removed, the cells are washed with PBS and fixed for 1 hour at 25°C adding a freshly made paraformaldheyde solution (4% in PBS). Samples are washed again with PBS and the endogenous oxidases were blocked for 2 minutes in the dark. Further washes with PBS followed and blocking the unspecific sites is done for 1 hour at 25℃. PARP is evidenced by immunolocalization utilizing a polyclonal antibody, directed against the N-terminal proteolytic fragment. Immuno-reaction is revealed by a secondary anti-rabbit antibody after incubation for 16 hours at 4°C. After exhaustive washing with PBS the samples are incubated for 30 minutes in solution ABC. Eventually, DAB (3,3'-Diaminobenzidine) is added and the samples are incubated for 10 minutes in the dark. The samples are washed again the plates are sealed and ready for microscopic observation. |
| Concentrations | 50 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Female nude mice |
| Formulation | |
| Dosages | 20 mg/kg |
| Administration | i.p. |
| Molecular Weight | 396.44 |
| Formula | C20H24N6O3 |
| CAS Number | 192705-79-6 |
| Solubility (25°C) | 14 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related FGFR Products |
|---|
| SNIPER(TACC3)-11
SNIPER(TACC3)-11 is a potent FGFR3-TACC3 degrader. |
| LY-3076226
LY-3076226 is an antibody drug coupling (ADC) with a cleavable linker targeting FGFR2. |
| Aprutumab ixadotin
Aprutumab ixadotin is an antibody drug coupling (ADC) with a non-cleavable linker that targets FGFR2. |
| Gunagratinib
Gunagratinib is an orally active, potent, selective, and irreversible fibroblast growth factor receptor (pan-FGFR) inhibitor for use in cancer research. |
| SAR-442501
SAR-442501 is a novel anti-FGFR3 monoclonal antibody for studies related to achondroplasia (ACH). |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
