Potent PDGFR family inhibitor (IC50
values are 1.2, 2, 7.7 and 10.5 nM for KIT, FLT3, PDGFRβ
and CSF1R respectively; Kd
= 1.3 nM for PDGFRα
). Exhibits >30-fold selectivity over a panel of other kinases and exhibits no activity against cytochrome P450. Causes tumor regression of leukemia cell xenografts in mice. Also reduces joint swelling and inflammation in a mouse model of collagen-induced arthritis. Orally active.
Soluble to 20 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.
Discovery of AC710, a globally selective inhibitor of platelet-derived growth factor receptor-family kinases.
Liu et al.
ACS Med.Chem.Lett., 2012;3:997