| Description : |
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. |
| Form : |
Solid, White to light yellow |
| Target : |
Src; Apoptosis |
| In Vitro : |
A419259 is a second-generation pyrrolopyrimidine that can block the proliferation of CML cell lines and induce apoptosis. It induces apoptosis in K-562 cells and inhibits the proliferation of Meg-01 (IC50 = 0.1 μM).
In the absence of IL-3, A-419259 strongly inhibits the proliferation of DAGM/Bcr-Abl cells (IC50 = 0.1-0.3 μM).
A-419259 also inhibits overall SFK activity in CML cell lines and can block the activation of Src kinase (IC50 = 0.1-0.3 μM).
A 419259 GMP (1 μM; 16 h) inhibits the activity of endogenous SFK (c-Src and Lck), thereby inhibiting Src-driven differentiation of mES cells into primitive ectoderm-like cells.
A 419259 GMP (0.3, 1 μM; 5 days) has no effect on the undifferentiated colony morphology of hES cells grown in mTeSR medium. |
| Solubility Data : |
DMSO: 100 mg/mL (207.20 mM; Need ultrasonic and warming) |
| IC50 & Target : |
IC50: 9 nM (Src), <3 nM (Lck), <3 nM (Lyn), 3 μM (Abl) |
| CAS : |
364042-47-7 |
| Formula : |
C29H34N6O |
| Molecular Mass : |
482.63 |
| Storage : |
4 centigrade, sealed storage, away from moisture and light |
