Bosutinib is an ATP-competitive dual Src/Abl kinase inhibitor (IC50 = 1 nM). It potently inhibits the apoptosis-linked STE20 kinases but does not inhibit Kit or PDGFR. Bosutinib was found to inhibit 16 of 18 imatinib-resistant mutant forms of Bcr-Abl expressed in murine myeloid cell lines, but...
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Bosutinib is an ATP-competitive dual Src/Abl kinase inhibitor (IC50 = 1 nM). It potently inhibits the apoptosis-linked STE20 kinases but does not inhibit Kit or PDGFR. Bosutinib was found to inhibit 16 of 18 imatinib-resistant mutant forms of Bcr-Abl expressed in murine myeloid cell lines, but did not inhibit T315I and V299L mutants. Enhances retinoic acid-induced differentiation of HL-60 leukemia cells. Suppresses migration and invasion of human breast cancer cells (IC50 = 250 nM which is also the IC50 for inhibition of cellular Src kinase activity in intact tumor cells)
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