Cayman A-419259 (Hydrochloride); Purity- Greater Than Or Equal To

A-419259 is an inhibitor of Src family kinases, including Src, LCK, Lyn, and Hck (IC₅₀s = 9, <3, <3, and 11.26 nM, respectively).^1,2 It is selective for these kinases over c-Abl (IC₅₀ = 3,000 nM) and PKC (IC₅₀ = >33 μM).¹ A-419259 inhibits growth of Philadelphia chromosome-positive (Ph⁺) K-562 and Meg-01 myeloid leukemia cells (IC₅₀s = 0.1-0.3 and 0.1 μM, respectively), but not Ph^- TF-1 and HEL cells. It induces apoptosis in K-562 cells in a concentration-dependent manner. A-419259 (300 nM) inhibits differentiation of murine embryonic stem cells while maintaining pluripotency.³ It reduces the total number of acute myeloid leukemia (AML) cells, as well as AML stem cells, in the bone marrow and spleen in mouse patient-derived xenograft (PDX) models of AML when administered at a dose of 30 mg/kg twice daily.⁴

WARNING This product is not for human or veterinary use.