Chemical Name: 6-(2,6-Dichlorophenyl)-2-[(4-fluoro-3-methylphenyl)amino]-8-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
Biological ActivityATP-competitive inhibitor of p210bcr/abl tyrosine kinase; selectively induces apoptosis in chronic myeloid leukemia (CML) K562 cells. Inhibits in vivo tyrosine phosphorylation of Gab2, CrkL and p210bcr/abl (IC50 values are 80, 80 and 170 nM respectively). Potently inhibits p210bcr/abl autophosphorylation in vitro (IC50 = 5 nM). Also potently inhibits c-Src and KIT (IC50 values are 0.8 and 50 nM, respectively).
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For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
The pyrido[2,3-d]pyrimidine derivative PD180970 inhibits p210bcr-abl tyrosine kinase and induces apoptosis of K562 leukemic cells.
Dorsey et al.
Cancer Res., 2000;60:3127
Sensitivity of oncogenic KIT mutants to the kinase inhibitors MLN518 and PD180970.
Corbin et al.
Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to ima. mesylate (Gleevec, STI571).
La Rosée et al.
Cancer Res., 2002;62:7149
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