Potent PI 3-Kinase δ isoform inhibitor
Idelalisib is a potent PI 3-Kinase δ inhibitor (IC50 = 2.5 nM for p110δ); it exhibits >40-fold selectivity for the δ isoform over other PI 3-K class I enzymes (IC50s = 89, 565, and 820 nM for p110γ, p110β, and p110α respectively). Idelalisib blocks constitutive PI 3-K signaling in malignant B-cell lines and primary patient tumor cells. Idelalisib inhibits chronic lymphocytic leukemia cell chemotaxis and downregulates chemokine secretion triggered by B-cell receptor signaling in stromal cocultures. Idelalisib lacks significant cytotoxicity toward natural killer (NK) cells. Idelalisib also decreases production of inflammatory cytokines, including TNF-γ, CD40L, and IL-6 by T cells and IFN-γ by NK cells. Idelalisib is cell-permeable and orally bioavailable.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-124570 |
| Réf. fabricant | 18749626 |
| Nom chimique ou matériau | 5-Fluoro-3-phenyl-2-[(1 S)-1-(9 H-purin-6-ylamino)propyl]-4(3 H)-quinazolinone |
| CAS | 870281-82-6 |
| Quantité | 10 mg |
| Cible | PI 3-Kinase Inhibitors |
| Formule moléculaire | C<sub>22</sub>H<sub>18</sub>FN<sub>7</sub>O |
| Pureté | 98% |
