Catalog No.: PC-60918Not For Human Use, Lab Use Only.
GNS-1486 is a novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 8.3, 4.2 and 4.3 nM for L858R-T790M, T790M and Del19-T790M, respectively.
GNS-1486 is a novel potent, irreversible, T790M mutant-selective inhibitor of mutant EGFR with IC50 of 8.3, 4.2 and 4.3 nM for L858R-T790M, T790M and Del19-T790M, respectively.
GNS-1486 displays >15-fold selectivity over wild type EGFR (IC50=121.6 nM) and L858R mutant (IC50=103.6 nM).
GNS-1486 demonstrates effectivity in multiple mouse xenograft models of human lung adenocarcinoma (T790M-positive or -negative), exhibiting less activity against wild-type EGFR than existing approved EGFR kinase inhibitors (including osimertinib).
GNS-1486 also shows superior potency against intracranial metastasis of EGFR-mutant lung adenocarcinoma.
