Bosutinib

Bosutinib is an inhibitor of c-Src and Abl kinases (IC₅₀s = 1.2 and 1 nM, respectively).^1,2 It also inhibits the kinases EPHB2, TrkA, TrkB, and TXK (IC₅₀s = 8.5, 22, 27, and 40 nM, respectively) among others.³ Bosutinib inhibits Src-dependent cell proliferation (IC₅₀ = 100 nM) and reverses Src-transformed fibroblasts to a non-transformed morphology when used at a concentration of 1 µM.¹ It reduces tumor growth in unstaged and staged Src-transformed fibroblast mouse xenograft models when administered at doses of 30 or 25 mg/kg, respectively, twice per day. Bosutinib (100 mg/kg) also induces complete tumor regression in a K562 mouse xenograft model when administered once per day for five days.²

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1. Boschelli, D.H., Ye, F., Wang, Y.D., et al. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity. J. Med. Chem. 44, 3965-3977 (2001).

2. Golas, J.M., Arndt, K., Etienne, C., 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. 63(2), 375-381 (2003).

3. Remsing Rix, L.L., Rix, U., Colinge, J., et al. Global target profile of the kinase inhbitor bosutinib in primary chronic myeloid leukemia cells. Leukemia 23, 477-485 (2009).