| MDL | - |
|---|---|
| Molecular Weight | 592.00 |
| Molecular Formula | C29H37Cl3N6O |
| SMILES | NC1=C2C(N([C@H]3CC[C@H](N4CCN(C)CC4)CC3)C=C2C5=CC=C(OC6=CC=CC=C6)C=C5)=NC=N1.[H]Cl.[H]Cl.[H]Cl |
IC50: 9 nM (Src), <3 nM (Lck), <3 nM (Lyn), 3 μM (Abl) [1]
A 419259 Trihydrochloride 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 IC 50 between 0.1 and 0.3 μM, and Meg-01 proliferation with an IC 50 of 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 IC 50 between 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 IC 50 between 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 IC 50 value of 0.1-0.3 μM [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Solid
Room temperature in continental US; may vary elsewhere.
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
H 2 O : ≥ 55 mg/mL ( 92.91 mM )
DMSO : 1 mg/mL ( 1.69 mM ; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6892 mL | 8.4459 mL | 16.8919 mL |
| 5 mM | 0.3378 mL | 1.6892 mL | 3.3784 mL |
| 10 mM | 0.1689 mL | 0.8446 mL | 1.6892 mL |
Add each solvent one by one: PBS
Solubility: 100 mg/mL (168.92 mM); Clear solution; Need ultrasonic