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Osimertinib-13C,d3

Names

[ CAS No. ]:
2254100-49-5

[ Name ]:
Osimertinib-13C,d3

Biological Activity

[Description]:

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.

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> EGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[In Vitro]

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].

[References]

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

[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

Chemical & Physical Properties

[ Molecular Formula ]:
C2713CH30D3N7O2

[ Molecular Weight ]:
503.62

Related Compounds