A 419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, designed to enhance selectivity towards theSrcfamily withIC₅₀of 9 nM,<3 nm and<3 forSrc,LckandLyn, respectively.

IC50: 9 nM (Src),<3 nm (lck),<3 (lyn), 3 μm (abl)^[1]

A 419259 is a second-generation pyrrolo-pyrimidine designed to enhance selectivity towards the Src family relative to other cytoplasmic tyrosine kinases. A-419259 inhibits K-562 cells with an IC₅₀between 0.1 and 0.3 μM, and Meg-01 proliferation with an IC₅₀of approximately 0.1 μM. A-419259 also potently induces apoptosis in K-562 cells beginning at 0.1 μM and increasing in a dose-dependent manner. PP2 inhibits Src kinase autophosphorylation in both Ph⁺cell lines (K-562 and Meg-01) with an IC₅₀between 3 and 10 μM, while A-419259 blocks kinase activation between 0.1 and 0.3 μM. A-419259 strongly inhibits DAGM/Bcr-Abl cell proliferation in the absence of IL-3 with an IC₅₀between 0.1 and 0.3 μM^[1]. A-419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, and blocks proliferation and induces apoptosis in CML cell lines. A-419259 inhibits overall SFK activity in K562 and other CML cell lines with an IC₅₀value of 0.1-0.3 μM^[2].

482.62

C₂₉H₃₄N₆O

364042-47-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.