NCIt definition : An orally bioavailable small molecule 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 IDRX-42 targets, binds to and inhibits specific
c-Kit mutants. 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.;