ALM301 (ALM-301) is a potent, selective and allosteric inhibitor of AKT1 and AKT2 with IC50 of 125 nM and 95 nM respectively.
ALM301 demonstrates excellent selectivity against 450 kinases at 10 uM.
ALM301 inhibits proliferation in a cancer cell line panel. MCF-7 cells, containing a PI3KCA mutation, is among the most sensitive with IC50 of 2.25 uM.
ALM301 inhibits AKT phosphorylation and modulates downstream signalling in vitro.
ALM301 orally dosed at 10, 30 and 100 mg/kg q.d. or q.o.d. showed significant anti-tumour efficacy in an A549 lung cancer xenograft.
