CAS: 1001083-74-4

APCK-110 is a tyrosine kinase inhibitor that has been shown to inhibit the constitutive activation of the mastocytosis receptor tyrosine kinase, KIT. APCK-110 has also demonstrated efficacy in clinical studies involving patients with leukemia who were resistant to imatinib and dasatinib. The drug inhibits proliferation of cancer cells, and may also be able to differentiate between leukemias and stem cells. The drug has been shown to have toxicities, such as anemia, neutropenia, thrombocytopenia, and hepatotoxicity. These toxicities are dose-dependent, with the most severe side effects seen at high doses.

"APcK110, a potent novel Kit inhibitor, outperforms imatinib/dasatinib in halting OCI/AML3 and HMC1.2 cell growth, also inhibiting Kit-signaling."