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Carfilzomib-d8

Names

[ CAS No. ]:
1537187-53-3

[ Name ]:
Carfilzomib-d8

[Synonym ]:
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]-

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
975.6±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C40H49D8N5O7

[ Molecular Weight ]:
727.96

[ Flash Point ]:
543.8±34.3 °C

[ Exact Mass ]:
727.476013

[ LogP ]:
6.71

[ Vapour Pressure ]:
0.0±0.3 mmHg at 25°C

[ Index of Refraction ]:
1.551

Related Compounds