ATP-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
values are 80, 80 and 170 nM respectively). Potently inhibits p210bcr/abl
autophosphorylation in vitro
= 5 nM). Also potently inhibits c-Src and KIT (IC50
values are 0.8 and 50 nM, respectively).
Soluble to 50 mM in DMSO
Store at +4°C
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Sold for research purposes under agreement from Pfizer Inc.
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 imatinib mesylate (Gleevec, STI571).
La Rosée et al.
Cancer Res., 2002;62:7149