DCC2036, also known as Rebastinib, is a multi-targeted kinase inhibitor primarily utilized in oncology. It potently inhibits the TIE2 kinase receptor, which is crucial for angiogenesis (new blood vessel formation), as well as BCR-ABL kinase (including the resistant T315I mutant), playing key roles in tumor growth, metastasis, and leukemia cell survival.

In solid tumors, Rebastinib disrupts angiogenesis-dependent signaling pathways, showing promise in reducing tumor growth and spread in cancers such as breast cancer and glioblastoma. It is often studied in combination with other anticancer agents to enhance efficacy and overcome resistance. Additionally, its BCR-ABL inhibition makes it valuable for treating chronic myeloid leukemia (CML), particularly cases resistant to other tyrosine kinase inhibitors.

Clinical trials explore its use across various malignancies, including potential applications in acute myeloid leukemia (AML), though primary focus remains on CML and angiogenesis-driven solid tumors. By modulating the tumor microenvironment and key signaling pathways, Rebastinib aims to improve patient outcomes in advanced cancers with limited treatment options.