PD 166866 Property

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

Hazard Codes 

Xn

Risk Statements 

22

WGK Germany 

1

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

PD 166866 Chemical Properties,Usage,Production

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.