Rebastinib (formerly also known as DCC-2036), a novel, potent and orally bioavailable small-molecule inhibitor of multiple tyrosine kinases with potential antineoplastic activity, is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50s of 0.8 nM and 4 nM. It also inhibits other kinases such as SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and has low activity towards c-Kit. DCC-2036 inhibits ABL1 through forcing the kinase domains into inhibitor-bound, inactive Type II conformations. In cellular assay, DCC-2036 inhibits the proliferation of Ba/F3 and K562 cells with IC50 values of 5.4nM and 5.5nM, respectively.