Potent irreversible proteasome inhibitor; active in vivo
Carfilzomib is a potent irreversible proteasome inhibitor. Preferentially inhibits the chymotrypsin-like β5 subunit of the constitutive 20S proteasome (IC50 = 5.2 nM) and the β5i subunit of the immunoproteasome 20Si (LMP7; IC50 = 14 nM)
in vitro
with minimal cross-reactivity to other proteases. Exhibits little or no effect on PGPH and T-L activities. Activates prosurvival autophagy and induces cell apoptosis. Acts synergistically with dexamethasone (Cat. No. 1126). Suppresses tumor growth in an
xenograft model. Decreases bone resorption and enhances bone formation in non-tumor bearing mice.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-158026 |
| Réf. fabricant | 18737066 |
| Nom chimique ou matériau | (αS)-α-[[2-(4-Morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1 S)-3-methyl-1-[[(2 R)-2-methyl-2-oxiranyl]carbonyl]butyl]-L-phenylalaninamide |
| CAS | 868540-17-4 |
| Quantité | 50 mg |
| Cible | Proteasome Inhibitors |
| Formule moléculaire | C<sub>40</sub>H<sub>57</sub>N<sub>5</sub>O<sub>7</sub> |
| Pureté | 0.98 |
