Bosutinib是一種口服Src/Abl酪氨酸激酶抑制劑,IC50分別為1.2 nM和1 nM。
Bosutinib (SKI-606) is an active inhibitor of Bcr-Abl in several chronic myelogenous leukemia cell lines, with IC50 values in the low nanomolar range[2].
Bosutinib (oral gavage; 75 mg/kg twice daily or 150 mg/kg once daily) has activity against human KU812 xenografts in nude mice. Bosutinib (150 mg/kg; once daily, 5 days weekly) has activity against syngeneic Bcr-Abl WT and mutant Ba/F3 xenografts[2].
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