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PD166326

Names

[ CAS No. ]:
185039-91-2

[ Name ]:
PD166326

[Synonym ]:
Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-(2,6-dichlorophenyl)-2-[[3-(hydroxymethyl)phenyl]amino]-8-methyl-
6-(2,6-Dichlorophenyl)-2-{[3-(hydroxymethyl)phenyl]amino}-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one

Biological Activity

[Description]:

PD166326 is a pyridopyrimidine-type inhibitor of receptor tyrosine kinases, with IC50s of 6 nM and 8 nM for Src and Abl, respectively. PD166326 exhibits antileukemic activity[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Src
Signaling Pathways >> Membrane Transporter/Ion Channel >> BCRP

[Target]

IC50: 6 nM (Src), 8 nM (Abl)[1]


[References]

[1]. Huron DR, et, al. A novel pyridopyrimidine inhibitor of abl kinase is a picomolar inhibitor of Bcr-abl-driven K562 cells and is effective against STI571-resistant Bcr-abl mutants. Clin Cancer Res. 2003 Apr;9(4):1267-73.

[2]. Wolff NC, et, al. PD166326, a novel tyrosine kinase inhibitor, has greater antileukemic activity than imatinib mesylate in a murine model of chronic myeloid leukemia. Blood. 2005 May 15;105(10):3995-4003.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
646.3±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C21H16Cl2N4O2

[ Molecular Weight ]:
427.283

[ Flash Point ]:
344.7±34.3 °C

[ Exact Mass ]:
426.065033

[ PSA ]:
80.04000

[ LogP ]:
3.04

[ Vapour Pressure ]:
0.0±2.0 mmHg at 25°C

[ Index of Refraction ]:
1.706

Related Compounds