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

Safety Information

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; K_i = 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).

Definition

ChEBI: PD-166866 is a member of the class of pyridopyrimidines that is pyrido[2,3-d]pyrimidine substituted by an amino group at position 2, 3,5-dimethoxyphenyl group at position 6, and by a (tert-butylcarbamoyl)nitrilo group at position 7. It is a selective ATP competitive inhibitor of the human fibroblast growth factor-1 receptor (FGFR1) tyrosine kinase with an IC50 of 52.4 nM. It has a role as an apoptosis inducer, an antineoplastic agent, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor and an angiogenesis inhibitor. It is a dimethoxybenzene, a pyridopyrimidine, a member of ureas, a biaryl and a primary arylamine.

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.

References

[1] R L PANEK. In vitro biological characterization and antiangiogenic effects of PD 166866, a selective inhibitor of the FGF-1 receptor tyrosine kinase.[J]. Journal of Pharmacology and Experimental Therapeutics, 1998, 286 1: 569-577.
[2] HENDRIK FISCHER. Fibroblast growth factor receptor-mediated signals contribute to the malignant phenotype of non-small cell lung cancer cells: therapeutic implications and synergism with epidermal growth factor receptor inhibition.[J]. Molecular Cancer Therapeutics, 2008, 7 10: 3408-3419. DOI: 10.1158/1535-7163.mct-08-0444

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