PD166326

PD166326 is an orally active tyrosine kinase inhibitor with a IC₅₀ of 8 nM against abl tyrosine kinase and a IC₅₀ of 6 nM against src tyrosine kinase. PD166326 blocks Bcr/Abl kinase activity. PD166326 inhibits Bcr/Abl-dependent proliferation and cell cycle progression. PD166326 reduces peripheral blood granulocytosis, alleviates splenomegaly and prolongs survival in a mouse model of chronic myeloid leukemia. PD166326 can be used in research related to chronic myeloid leukemia^[1][2]. IC50 & Target:IC50: 6 nM (Src), 8 nM (Abl)^[1] In Vitro:PD166326 (0.1-2.5 nM; 48 h) potently inhibits Bcr/Abl-dependent proliferation of R10(-) cells, with an IC₅₀ of 0.2 nM^[1].
PD166326 (5-50 nM; 48 h) inhibits stem cell factor-dependent proliferation of parental MO7E cells, with an IC₅₀ of 12 nM^[1].
PD166326 (10 min; 30°C) potently inhibits purified recombinant c-abl tyrosine kinase in vitro with an IC₅₀ of 8 nM^[2].
PD166326 potently inhibits purified recombinant c-src tyrosine kinase in vitro with an IC₅₀ of 6 nM^[2].
PD166326 (4-7 days) potently inhibits the growth of K562 Bcr-abl-positive cells with an IC₅₀ of 0.3 nM^[2].
PD166326 (4-7 days) potently inhibits the growth of BaF3 p210Bcr-abl Bcr-abl-positive cells with an IC₅₀ of 6.0 nM^[2]. In Vivo:PD166326 (50 mg/kg; p.o.; twice a day) provides better control of the murine CML-like illness than Imatinib
mesylate (HY-50946)^[1].