Carfilzomib-d8

Carfilzomib-d8 is deuterium labeled Carfilzomib. Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.

O=C([C@@H](NC([C@H](CC1=CC=CC=C1)NC([C@H](CC(C)C)NC([C@@H](NC(CN2C([2H])(C([2H])(OC([2H])(C2([2H])[2H])[2H])[2H])[2H])=O)CCC3=CC=CC=C3)=O)=O)=O)CC(C)C)[C@@]4(OC4)C

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.|[2]Dasmahapatra G, et al. Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells in vitro and in vivo. Mol Cancer Ther. 2011 Sep;10(9):1686-97.|[3]Kuhn DJ, et al. Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. Blood. 2007 Nov 1;110(9):3281-90.