DS-1205b (DS1205b) is a potent, highly selective inhibitor of AXL kinase with IC50 of 1.3 nM.
DS-1205b displays 48-, 80-, and 313-fold selectivity ovver MER, MET, and TRKA.
DS-1205b inhibits phosphorylation of AKT serine/threonine kinase in a dose-dependent manner.
DS-1205b does not obviously inhibit cell proliferation and viability in NIH3T3-AXL cells.
DS-1205b significantly suppresses cell migration on NIH3T3-AXL with IC50 of 2.7 nM.
DS-1205b induces tumor regression by 54-86% at doses of 6.3-50 mg/kg in mice bearing subcutaneously implanted NIH3T3-AXL cells.
DS-1205b inhibits AXL signaling in vitro when combined with erlotinib or osimertinib, delays erlotinib acquired resistance and restores the treatment effect of erlotinib in an HCC827 sc xenograft model.
