Bosutinib-d₈  (Synonyms: SKI-606-d₈)

Bosutinib-d₈ is a deuterium labeled Bosutinib. Bosutinib is a dual Src/Abl inhibitor with IC₅₀s of 1.2 nM and 1 nM, respectively^[1][2].

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.

IC50: 1.2 nM (Src), 1 nM (Abl)^[1]

538.50

C₂₆H₂₁D₈Cl₂N₅O₃

380843-75-4

Solid

White to off-white

CN1C([2H])([2H])C([2H])([2H])N(C([2H])([2H])C1([2H])[2H])CCCOC2=C(C=C3C(NC4=CC(OC)=C(C=C4Cl)Cl)=C(C=NC3=C2)C#N)OC

Room temperature in continental US; may vary elsewhere.

• [1]. Boschelli DH, et al. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J Med Chem, 2001, 44(23), 3965-3977.  [Content Brief]

  [2]. Golas JM, et al. SKI-606, a 4-anilino-3-quinolinecarbonitrile dual inhibitor of Src and Abl kinases, is a potent antiproliferative agent against chronic myelogenous leukemia cells in culture and causes regression of K562 xenografts in nude mice. Cancer Res, 2003, 63(2), 375-381.  [Content Brief]