EP102 is a potent, selective METTL3 inhibitor with IC50 of 2 nM in SPA primary assay.
EP102 showed nanomolar potency across a broad panel of cancer cell lines (Kasumi-1 (IC50=61 nM) and MV-4-11 (AML), Calu-6 and A549 (lung), FaDu (head and neck), and Caov-3 and SK-OV-3 (ovarian)).
EP102 potently inhibits intracellular m6A in SK-OV-3 cells with IC50 of 6 nM,.
EP102 selectively inhibits METTL3/14 among a panel of 40 methyl transferases.
EP102 demonstrated a dose-dependent inhibition of m6A up to a maximum reduction (79%) following a single dose of 3 mg/kg (oral) in PBMCs from rats.
EP102 (20 mg/kg, po, QD) inhibited tumor growth in AML xenograft model (MV-4-11-Luc-mCh-Puro CDX model).
