Ribociclib-d8

Modify Date: 2024-01-17 11:02:22

Ribociclib-d8 Structure
Ribociclib-d8 structure
Common Name Ribociclib-d8
CAS Number 2167898-24-8 Molecular Weight 442.59
Density N/A Boiling Point N/A
Molecular Formula C23H22D8N8O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Ribociclib-d8


Ribociclib-d8 is the deuterium labeled Ribociclib[1]. Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[2].

 Names

Name Ribociclib-d8

 Ribociclib-d8 Biological Activity

Description Ribociclib-d8 is the deuterium labeled Ribociclib[1]. Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex[2].
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 Feb;53(2):211-216.  

[2]. VanArsdale T, et al. Molecular Pathways: Targeting the Cyclin D-CDK4/6 Axis for Cancer Treatment. Clin Cancer Res. 2015 Jul 1;21(13):2905-10.  

[3]. Rader J, et al. Dual CDK4/CDK6 Inhibition Induces Cell-Cycle Arrest and Senescence in Neuroblastoma. Clin Cancer Res. 2013 Nov 1519(22):6173-82.  

 Chemical & Physical Properties

Molecular Formula C23H22D8N8O
Molecular Weight 442.59