Abemaciclib metabolite M18-d8

Abemaciclib metabolite M18-d8 is the deuterium labeled Abemaciclib metabolite M18. Abemaciclib metabolite M18 (LSN3106729), the metabolite of Abemaciclib (HY-16297A), is a CDK inhibitor with antitumor activity. Abemaciclib metabolite M18 and a CRBN ligand have been used to design PROTAC CDK4/6 degrader[1][2].

Product Specifications

Product Name Alternative

LSN3106729-d8

UNSPSC

12352005

Target

CDK; Ligands for Target Protein for PROTAC

Type

Isotope-Labeled Compounds

Related Pathways

Cell Cycle/DNA Damage; PROTAC

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Purity

99.87

Solubility

DMSO : 32 mg/mL (ultrasonic)

Smiles

FC(C=N1)=C(C2=CC(N(C(C)C)C(CO)=N3)=C3C(F)=C2)N=C1NC4=NC=C(C=C4)CN5C([2H])([2H])C([2H])([2H])NC([2H])([2H])C5([2H])[2H]

Molecular Formula

C25H20D8F2N8O

Molecular Weight

502.59

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]Nathanael Gray, et al. Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use. WO2017185031A1.|[3]Edward S. Kim, et al. Abemaciclib in Combination with Single-Agent Options in Patients with Stage IV Non–Small Cell Lung Cancer: A Phase Ib Study.