6-(2,6-DICHLORO-PHENYL)-2-(4-FLUORO-3-METHYL-PHENYLAMINO)-8-METHYL-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE Chemical Properties

Boiling point:

590.6±60.0 °C(Predicted)

Density 

1.449±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: >20mg/mL

pka

3.02±0.20(Predicted)

form 

A solid

color 

yellow

Safety Information

Hazard Codes 

T

Risk Statements 

25

Safety Statements 

45

RIDADR 

UN 2811 6.1 / PGIII

WGK Germany 

3

6-(2,6-DICHLORO-PHENYL)-2-(4-FLUORO-3-METHYL-PHENYLAMINO)-8-METHYL-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE Usage And Synthesis

Uses

PD 180970 is an ATP-competitive inhibitor of p210 tyrosine kinase which selectively induces apoptosis in chronic myeloid leukemia (CML) K562 cells.

Biological Activity

PD-180970 is a potent inhibitor of the p210 Bcr-Abl tyrosine kinase.

in vivo

Enzyme inhibitor

This pyridopyrimidine (FWfree-base = 429.28 g/mol) inhibits Bcr-Abl proteintyrosine kinase and induces apoptosis of K562 leukemic cells. In vitro, PD180970 potently inhibited p210Bcr-Abl autophosphorylation (IC50 = 5 nM) as well as the kinase activity of purified Abl tyrosine kinase (IC50 = 2.2 nM). Incubation of K562 cells with PD180970 resulted in cell death, with results of nuclear staining, apoptotic-specific poly(ADP-ribose) polymerase cleavage, and annexin V binding assays confirming as much. Significantly, PD180970 is without effect on the growth and viability of p210Bcr-Ablnegative HL60 human leukemic cells. Such findings demonstrate that PD180970 is among the most potent known inhibitors of the p210Bcr-Abl tyrosine kinase and that it is a promising candidate as a novel therapeutic agent for Bcr-Abl-positive leukemia

IC 50

Bcr-Abl: 5 nM (IC₅₀, p210^Bcr-Abl kinase); Src: 0.8 nM (IC₅₀); KIT: 50 nM (IC₅₀)

6-(2,6-DICHLORO-PHENYL)-2-(4-FLUORO-3-METHYL-PHENYLAMINO)-8-METHYL-8H-PYRIDO[2,3-D]PYRIMIDIN-7-ONE(287204-45-9)Related Product Information

• 2,6-DICHLOROPHENYLACETAMIDE
• PD180970