Chemical Name: 4-[(2,4-Dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile
Biological ActivityBosutinib 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.
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Optimization of 4-phenylamino-3-quinolinecarbonitriles as potent inhibitors of Src kinase activity.
Boschelli 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.
Golas et al.
Cancer Res., 2003;63:375
SKI-606, a Src/Abl inhibitor with in vivo activity in colon tumor xenograft models.
Golas et al.
Cancer Res., 2005;65:5358
SKI-606 (bosutinib), a novel Src kinase inhibitor, suppresses migration and invasion of human breast cancer cells.
Vultur et al.
Citations for Bosutinib
The citations listed below are publications that use Tocris products. Selected citations for Bosutinib include:
2 Citations: Showing 1 - 2
A conserved water-mediated hydrogen bond network defines bosutinib's kinase selectivity.
Nat Chem Biol 2014;10:127
Structural and spectroscopic analysis of the kinase inhibitor bosutinib and an isomer of bosutinib binding to the Abl tyrosine kinase domain.
Authors: Levinson and Boxer
PLoS One 2012;7:e29828
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