Bosutinib

Biological Activity

Bosutinib is a dual inhibitor of Abl and Src kinases (IC₅₀ = 1.2 nM for Src in an enzymatic assay). Displays antiproliferative activity against chronic myelogenous leukemia (CML) cells and decreases the motility and invasion of breast cancer cell lines. Also exhibits potent antiproliferative activity in anchorage-independent, Src-transformed rat fibroblasts (IC₅₀ = 100 nM). Displays selectivity for Src over non-Src family kinases such as growth factor receptor tyrosine kinases.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Background References

1. Structural and spectroscopic analysis of the kinase inhibitor bosutinib and an isomer of bosutinib binding to the Abl tyrosine kinase domain.
   Levinson NM, Boxer SG
   PLoS ONE, 2012;7(4):e29828.
2. Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity.
   Boschelli et al.
   J.Med.Chem., 2001;44:3965
3. 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.
   Golas et al.
   Cancer Res., 2003;63:375
4. SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models.
   Golas et al.
   Cancer Res., 2005;65:5358
5. SKI-606 (bosutinib), a novel Src kinase inhibitor, suppresses migration and invasion of human breast cancer cells.
   Vultur et al.
   Mol.Cancer.Ther., 2008;7:1185

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