Bioactivity | Abemaciclib metabolite M2-d6 is the deuterium labeled Abemaciclib metabolite M2. Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50s in the range of 1-3 nM. Anti-cancer activity[1][2]. |
Invitro | 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]. |
Name | Abemaciclib metabolite M2-d6 |
Formula | C25H22D6F2N8 |
Molar Mass | 484.58 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | -20°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
Reference | [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Teresa Burke, et al. Abstract 2830: The major human metabolites of abemaciclib are inhibitors of CDK4 and CDK6. Cancer Research. July 2016, 76 (14). |