EEDi-5285 (C09-1130-574)

EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC 50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activityIn VitroEEDi-5285 inhibits cell growth with IC 50 values of 20 pM and 0.5 nM in the Pfeiffer and KARPAS422 lymphoma cell lines, respectively, carrying an EZH2 mutation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoEEDi-5285 (compound 28; 50-100 mg/kg; oral gavage; daily; for 28 days; SCID mice) treatment achieves complete and durable tumor regression in the KARPAS422 xenograft model in mice with oral administration . A single 100 mg/kg oral administration of EEDi-5285 (compound 28) effectively reduces the level of H3K27me3 at 24 h in KARPAS422 tumor tissue in mice . EEDi-5285 (compound 28) achieves a C max of 1.8 μM and an AUC of 6.0 h▪μg/ml with 10 mg/kg oral administration and has an oral bioavailability (F) of 75%. EEDi-5285 has a moderate volume of distribution of 1.4 L/kg and a terminal T 1/2 of approximately 2 h . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice injected with KARPAS422 cells Dosage: 50 mg/kg, 100 mg/kg Administration: Oral gavage; daily; for 28 days Result: Showed highly efficacious and capable of achieving complete and long-lasting tumor regression in the KARPAS422 xenograft model in mice with oral administration.Form:SolidIC50& Target:IC50: 0.2 nM (Embryonic ectoderm development (EED)). Specification: 0.99 Molecular Formula: C24H22FN5O3S Molecular Weight: 479.53