Ruxolitinib-d₉  (Synonyms: INCB18424-d₉)

Ruxolitinib-d₉ (INCB18424-d₉) is deuterium labeled Ruxolitinib. Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC₅₀s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3^[1]. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy^[3].

1. This compound can be used as a tracer.
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

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.

315.42

C₁₇H₉D₉N₆

1513883-55-0

941678-49-5

N#CC[C@H](C1([2H])C([2H])([2H])C([2H])([2H])C([2H])([2H])C1([2H])[2H])N2C=C(C=N2)C3=C4C(NC=C4)=NC=N3

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 Feb;53(2):211-216.  [Content Brief]

  [2]. Verstovsek S, et al. A double-blind, placebo-controlled trial of ruxolitinib for myelofibrosis. N Engl J Med, 2012, 366(9), 799-807.  [Content Brief]

  [3]. Quintas-Cardama A, et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood, 2010, 115(15), 3109-3117.  [Content Brief]

  [4]. Tavallai M, et al. Rationally Repurposing Ruxolitinib (Jakafi (®)) as a Solid Tumor Therapeutic.Front Oncol. 2016 Jun 13;6:142.  [Content Brief]