192705-79-6
192705-79-6 structure
- Name: PD-166866
- Chemical Name: 1-[2-amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-3-tert-butylurea
- CAS Number: 192705-79-6
- Molecular Formula: C20H24N6O3
- Molecular Weight: 396.44300
- Catalog: Research Areas Cancer
- Create Date: 2016-02-22 17:44:55
- Modify Date: 2024-01-02 21:03:03
-
PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC50 of 52.4 nM.
| Name | 1-[2-amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-3-tert-butylurea |
|---|---|
| Synonyms |
1-[2-Amino-6-(3,5-dimethoxyphenyl)-pyrido[2,3-d]pyrimidin-7-yl]-3-tert-butyl urea
HIF-1alpha HMS3263L17 PD-166866 PD166866 |
| Description | PD166866 is a selective FGFR1 tyrosine kinase inhibitor with an IC50 of 52.4 nM. |
|---|---|
| Related Catalog | |
| Target |
FGFR1:52.4 nM (IC50) |
| In Vitro | PD 166866 inhibits human full-length FGFR-1 tyrosine kinase with an IC50 value of 52.4 nM and is characterized as an ATP competitive inhibitor of the FGFR-1. PD 166866 is a potent inhibitor of FGFR autophosphorylation in NIH 3T3 cells expressing endogenous FGFR-1 and in L6 cells overexpressing the human FGFR-1 tyrosine kinase. PD 166866 also inhibits bFGF-induced tyrosine phosphorylation of the 44- and 42-kDa (ERK 1/2) mitogen-activated protein kinase isoforms in L6 cells. Daily exposure of PD 166866 to L6 cells at concentrations from 1 to 100 nM results in a concentration-related inhibition of bFGF-stimulated cell growth for 8 consecutive days with an IC50 value of 24 nM[1]. |
| Cell Assay | PD 166866 is dissolved in DMSO. PD 166866 or vehicle (0.5% DMSO, final concentration) are added every day to triplicate cultures of cells together with 25 ng/mL bFGF to stimulate FGF-driven growth. In some experiments, PD 166866 is added every day to triplicate cultures of cells together with 30 ng/mL PDGF-BB to stimulate PDGF-driven growth. Cell number is measured by Coulter counting on days 1, 3, 6 or 8 after drug exposure[1] |
| References |
| Density | 1.277g/cm3 |
|---|---|
| Molecular Formula | C20H24N6O3 |
| Molecular Weight | 396.44300 |
| Exact Mass | 396.19100 |
| PSA | 128.50000 |
| LogP | 3.54580 |
| Index of Refraction | 1.643 |
| Storage condition | 2-8°C |
