The HCK/BTK Inhibitor KIN-8194 Is Active in MYD88 Driven Lymphomas and Overcomes Mutated BTKCys481 Ibrutinib Resistance

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Scientists performed an extensive medicinal chemistry campaign and identified KIN-8194 as a novel dual inhibitor of HCK and BTK. KIN-8194 showed potent and selective in vitro killing of MYD88 mutated lymphoma cells, including ibrutinib resistant BTKCys481Ser expressing cells.
[Blood]
Abstract