1537187-53-3

1537187-53-3 structure

Name: Carfilzomib-d8
Chemical Name: N-[(2S)-2-{[(2H8)-4-Morpholinylacetyl]amino}-4-phenylbutanoyl]-L-leucyl-N-{(2S)-4-methyl-1-[(2R)-2-methyl-2-oxiranyl]-1-oxo-2-pentanyl}-L-phenylalaninamide
CAS Number: 1537187-53-3
Molecular Formula: C₄₀H₄₉D₈N₅O₇
Molecular Weight: 727.96
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2018-07-15 14:49:22
Modify Date: 2024-01-09 11:55:52
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.

Name	N-[(2S)-2-{[(2H8)-4-Morpholinylacetyl]amino}-4-phenylbutanoyl]-L-leucyl-N-{(2S)-4-methyl-1-[(2R)-2-methyl-2-oxiranyl]-1-oxo-2-pentanyl}-L-phenylalaninamide
Synonyms	N-[(2S)-2-{[(2H8)-4-Morpholinylacetyl]amino}-4-phenylbutanoyl]-L-leucyl-N-{(2S)-4-methyl-1-[(2R)-2-methyl-2-oxiranyl]-1-oxo-2-pentanyl}-L-phenylalaninamide L-Phenylalaninamide, N-[(2S)-2-[[2-(4-morpholinyl-d8)acetyl]amino]-1-oxo-4-phenylbutyl]-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyloxiranyl]carbonyl]butyl]-

Description	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.
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome
In Vitro	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
References	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. 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. [3]. 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.