HKI-357

HKI-357 is a potent, irreversible small molecule inhibitor that targets both Receptor tyrosine-protein kinase erbB-2 (HER2) and Epidermal growth factor receptor (EGFR) tyrosine kinases. It exhibits low nanomolar inhibitory activity against these targets (IC50 values of 33 nM for Receptor tyrosine-protein kinase erbB-2 and 34 nM for Epidermal growth factor receptor). The drug suppresses ligand-induced Epidermal growth factor receptor autophosphorylation and cell proliferation in cancer cell lines harboring resistance mutations such as L858R and T790M in non-small-cell lung cancer. By inhibiting both Receptor tyrosine-protein kinase erbB-2 and Epidermal growth factor receptor, HKI-357 circumvents mechanisms of resistance to first-generation Epidermal growth factor receptor inhibitors like gefitinib (Iressa). It has been investigated in clinical trials for its safety, tolerability, and pharmacokinetics when administered orally to healthy subjects[1][3][4][5][6][8].

Other names

HKI 357HKI357HKI-357HKI-357 DIMALEATEHKI357 DIMALEATEHKI 357 DIMALEATE