Carfilzomib-d8

Modify Date: 2024-01-09 11:55:52

Carfilzomib-d8 Structure
Carfilzomib-d8 structure
Common Name Carfilzomib-d8
CAS Number 1537187-53-3 Molecular Weight 727.96
Density 1.2±0.1 g/cm3 Boiling Point 975.6±65.0 °C at 760 mmHg
Molecular Formula C40H49D8N5O7 Melting Point N/A
MSDS N/A Flash Point 543.8±34.3 °C

 Use of 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.

 Names

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
Synonym More Synonyms

 Carfilzomib-d8 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
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

 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]-