Osimertinib-¹³C,d₃  (Synonyms: AZD-9291-¹³C,d₃; Mereletinib-¹³C,d₃)

Osimertinib-¹³C,d₃ is the deuterium and ¹³C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.

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.

503.62

C₂₇¹³CH₃₀D₃N₇O₂

2254100-49-5

1421373-65-0

Solid

White to off-white

CN1C=C(C2=NC(NC3=C(C=C(C(NC(C=C)=O)=C3)N([13C]([2H])([2H])[2H])CCN(C)C)OC)=NC=C2)C4=CC=CC=C41

Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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

  [2]. Cross DA, et al. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014 Sep;4(9):1046-61.;Hirano T, et al. Pharmacological and Structural Characterizations of Naquotinib, a Novel Third  [Content Brief]