Crizotinib-d₉  (Synonyms: PF-02341066-d₉)

Crizotinib-d₉ (PF-02341066-d₉) is deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition^[1][2][3].

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.

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

459.39

C₂₁H₁₃D₉Cl₂FN₅O

1523580-59-7

877399-52-5

C[C@H](C1=C(C(F)=CC=C1Cl)Cl)OC2=CC(C3=CN(C4([2H])C([2H])([2H])C([2H])([2H])NC([2H])([2H])C4([2H])[2H])N=C3)=CN=C2N

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

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