Emilumenib (Menin-MLL inhibitor 26) is an orally active Menin-MLL inhibitor. Emilumenib also is an active reference. Emilumenib can inhibits cell growth. Emilumenib can be used for the research of leukemia [1].
In Vivo, Emilumenib (25-200 mg/kg, po for 24-35 days) reduces CD45 positive cells, exhibits anti-leukemic activity in xenograft mouse models[2].
In Vitro, Emilumenib (0-10 μM, 7 days) inhibits the menin-MLL1 interaction, exhibits cytotoxicity in acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) cells, that inhibits the cell growth of MLL or NPM1 mutated MV4-11, MOLM-13, OCI-AML3 and KOPN-8 with GI50s of 2.5, 6.2, 10 and 28.5 nM, respectively[2].
References:
[1]. Cycloalkane-1, 3-diamine derivatives, et al. Cycloalkane-1, 3-diamine derivatives. Patent. CN113164481A.
[2]. Numata M, et al., A novel Menin-MLL1 inhibitor, DS-1594a, prevents the progression of acute leukemia with rearranged MLL1 or mutated NPM1. Cancer Cell Int. 2023 Feb 25;23(1):36.
In Vivo, Emilumenib (25-200 mg/kg, po for 24-35 days) reduces CD45 positive cells, exhibits anti-leukemic activity in xenograft mouse models[2].
In Vitro, Emilumenib (0-10 μM, 7 days) inhibits the menin-MLL1 interaction, exhibits cytotoxicity in acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL) cells, that inhibits the cell growth of MLL or NPM1 mutated MV4-11, MOLM-13, OCI-AML3 and KOPN-8 with GI50s of 2.5, 6.2, 10 and 28.5 nM, respectively[2].
References:
[1]. Cycloalkane-1, 3-diamine derivatives, et al. Cycloalkane-1, 3-diamine derivatives. Patent. CN113164481A.
[2]. Numata M, et al., A novel Menin-MLL1 inhibitor, DS-1594a, prevents the progression of acute leukemia with rearranged MLL1 or mutated NPM1. Cancer Cell Int. 2023 Feb 25;23(1):36.