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].

Product Specifications

CAS Number

[2167898-24-8]

Product Name Alternative

LEE011-d8

UNSPSC

12352005

Hazard Statement

H301, H315, H319, H372, H400

Target

CDK

Type

Isotope-Labeled Compounds

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Purity

99.23

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CN(C)C(C(N(C1CCCC1)C2=N3)=CC2=CN=C3NC4=CC=C(N5C([2H])([2H])C([2H])([2H])NC([2H])([2H])C5([2H])[2H])C=N4)=O

Molecular Formula

C23H22D8N8O

Molecular Weight

442.59

Precautions

H301, H315, H319, H372, H400

References & Citations

[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.