Carfilzomib (PR171) (868540-17-4) Description:

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Carfilzomib (PR171) (868540-17-4) Description:

Carfilzomib (868540-17-4) is an epoxomicin derivate with potential antineoplastic activity. The mechanism of action of carfilzomib is as a Proteasome Inhibitor, Carfilzomib(PR171) irreversibly binds to and inhibits the chymotrypsin-like activity of the 20S catalytic core subunit of the proteasome, a protease complex responsible for degrading a large variety of cellular proteins. Inhibition of proteasome-mediated proteolysis results in an accumulation of polyubiquinated proteins, which may lead to cell cycle arrest, induction of apoptosis, and inhibition of tumor growth.

Carfilzomib (PR171) is used in treatment of refractory multiple myeloma. Carfilzomib(PR171) is associated with a low rate of serum enzyme elevations during treatment and has been implicated to rare instances of clinically apparent, acute liver injury some of which have been fatal.

Carfilzomib (PR171) is a second-generation, irreversible, peptide epoxyketone class proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.. It can induce cell cycle arrest and apoptosis in human cancer cell lines including multiple myeloma, lymphoma, and various solid tumors (IC50s = 2.4-20 nM).