KIT-mutant inhibitor DCC-3009

An orally bioavailable switch-control inhibitor of multiple mutated forms of mast/stem cell factor receptor KIT (c-Kit; SCFR), with potential antineoplastic activity. Upon oral administration, KIT-mutant inhibitor DCC-3009 targets and binds to the switch pocket of c-Kit, thereby inhibiting the activity of specific c-Kit mutants, including primary KIT mutations in exons 9 and 11 and secondary drug-resistant mutations across exons 13, 14, 17, and 18. This may inhibit tumor cell proliferation in cancer cell types that overexpress these c-Kit mutations. c-Kit, a transmembrane protein and receptor tyrosine kinase (RTK) overexpressed in various solid tumors and hematological malignancies, plays a key role in the regulation of cell differentiation and proliferation. Mutant forms of c-Kit are often associated with tumor chemoresistance.