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elenestinib

An orally bioavailable protein tyrosine kinase inhibitor of the mutated form of the tumor-associated antigen (TAA) mast/stem cell factor receptor c-Kit (SCFR), D816V, with potential antineoplastic activity. Upon oral administration, elenestinib binds to and inhibits the specific c-Kit mutant D816V. This may result in an inhibition of cell proliferation in mast cells that overexpress this c-Kit mutation. D816V, a mutation in which the amino acid asparagine aspartic acid at position 816 in the mast/stem cell growth factor receptor Kit protein is replaced by valine, may drive mastocytosis and other mast cell disorders.
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Synonym:D816V-mutant KIT inhibitor BLU-263
KIT D816V mutant-selective inhibitor BLU-263
Code name:BLU 263
BLU-263
BLU263
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