A 419259  (Synonyms: RK-20449)

A 419259 GMP is the GMP grade A 419259 (HY-15764), inducing cell apoptosis. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. A 419259 (RK-20449) is a broad-spectrum pyrrole-pyrimidine inhibitor targeting Src, Lck, and Lyn with IC₅₀s of 9 nM, <3 nM, and <3 nM, respectively^[1][2].

IC50: 9 nM (Src), <3 nM (Lck), <3 nM (Lyn), 3 μM (Abl)^[1]

A419259 is a second-generation pyrrolopyrimidine that blocks proliferation and induces apoptosis in CML cell lines. It induces apoptosis in K-562 cells and also inhibits Meg-01 proliferation (IC₅₀=0.1 μM)^[1].
In the absence of IL-3, A-419259 strongly inhibits DAGM/Bcr-Abl cell proliferation (IC₅₀=0.1-0.3 μM)^[1].
A-419259 also inhibits overall SFK activity in CML cell lines and blocks Src kinase activation (IC₅₀=0.1-0.3 μM)^[1].
A 419259 GMP (1 μM; 16 h) inhibits endogenous SFK (c-Src and Lck) activity, thereby inhibiting Src-driven differentiation of mES cells toward primitive ectoderm-like cells^[2].
A 419259 GMP (0.3, 1 μM; 5 days) has no effect on undifferentiated colony morphology of hES cells grown in mTeSR medium^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

482.62

C₂₉H₃₄N₆O

364042-47-7

NC1=C2C(N([C@H]3CC[C@H](N4CCN(C)CC4)CC3)C=C2C5=CC=C(OC6=CC=CC=C6)C=C5)=NC=N1

Room temperature in continental US; may vary elsewhere.

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

• [1]. Wilson MB, et al. Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr-Abl signal transduction and oncogenesis. Oncogene. 2002 Nov 21;21(53):8075-88.  [Content Brief]

  [2]. Zhang X, et al. Src-family tyrosine kinase activities are essential for differentiation of human embryonic stem cells. Stem Cell Res. 2014 Nov;13(3 Pt A):379-89.  [Content Brief]