Catalog No.: PC-47006Not For Human Use, Lab Use Only.
OBX02-011 is a potent, reversible, fourth-generation EGFR tyrosine kinase inhibitor (TKI) that overcomes the EGFR C797S mutation, inhibits triple mutants Del19/T790M/C797S and L858R/T790M/C797S with IC50 of 0.134 and 2.09 nM, respectively.
OBX02-011 is a potent, reversible, fourth-generation EGFR tyrosine kinase inhibitor (TKI) that overcomes the EGFR C797S mutation, inhibits triple mutants Del19/T790M/C797S and L858R/T790M/C797S with IC50 of 0.134 and 2.09 nM, respectively.
OBX02-011 occupied the ATP-binding site in a similar manner to WZ-4002.
OBX02-011 showed broad activity at low nanomolar concentrations against mutant EGFRs, more potent in Del19/T790M/C797S and L858R/T790M than in other EGFR mutations.
OBX02-011 was highly effective against EGFR triple mutations, and showed substantial selectivity compared with WT EGFR (IC50= 1471 nM in WT, 96.3 nM in Del19/T790M/C797S, and 94.8 nM in L858R/T790M/C797S) in Ba/F3 cell lines expressing EGFR.
OBX02-011 (25 mg/kg, i. p.) effectively inhibited tumor growth and EGFR activity, leading to enhanced survival in transgenic mouse models (EGFRL858R/T790M/C797S).
