Abemaciclib metabolite M2-d₆  (Synonyms: LSN2839567-d₆)

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

484.58

C₂₅H₂₂D₆F₂N₈

Solid

Off-white to light yellow

CC1=NC2=C(C=C(C3=C(C=NC(NC4=CC=C(C=N4)CN5CCNCC5)=N3)F)C=C2N1C(C([2H])([2H])[2H])C([2H])([2H])[2H])F

Room temperature in continental US; may vary elsewhere.

-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)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [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).