Description

Tandutinib is an inhibitor of several kinases, including FMS-like tyrosine kinase 3 (FLT3), PDGFR, and Kit. Tandutinib exhibits anticancer chemotherapeutic and anti-angiogenic activities and currently shows mixed results in clinical trials as a potential treatment for several cancers. In vivo, tandutinib inhibits phosphorylation of c-Kit, Akt, mTOR, and p70S6 kinase; it also increases activation of caspase 3 and the ratio of Bax/Bcl-2 and decreases expression of cyclin D1, resulting in apoptosis. In animal models, tandutinib decreases expression of COX-2 and VEGF, decreasing vessel formation and inhibiting growth of colon cancer xenografts. In an in vivo model of medulloblastoma, this compound decreases tumor volume.