Rebastinib tosylate (DCC-2036 tosylate) is an orally active, non-ATP-competitive Bcr-Abl inhibitor, with IC 50 values of 0.8 nM and 4 nM against Abl1 WT and Abl1 T315I , respectively. Rebastinib tosylate potently inhibits CYP2C8 ( IC 50 = 0.0533 μM) and CYP2C9 ( IC 50 = 2.54 μM). Rebastinib tosylate allosterically inhibits Tie2 with an IC 50 of 0.63 nM. Rebastinib tosylate inhibits the transcriptional activity of FoxO1 . Rebastinib tosylate inhibits SRC family kinases, KDR and FLT3 kinases. Rebastinib tosylate induces Apoptosis . Rebastinib tosylate exerts anti-tumor activity in breast cancer . Rebastinib tosylate exerts anti-angiogenic effects. Rebastinib tosylate increases myotube diameter and improves reduced contractility. Rebastinib tosylate can be used in research related to triple-negative breast cancer , luminal breast cancer , pancreatic neuroendocrine tumors, muscle atrophy, cancer cachexia, chronic myeloid leukemia, and B-lymphocytic leukemia.
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