Description
MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC 50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC 50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse.Appearance:SolidIn Vitro:MLT-231 (19.5-10000 nM) inhibits the proliferation of OCI-Ly3 cells. MLT-231 (50-5000 nM; 24 hours) leads to accumulation of the uncleaved form of its substrates CYLD, BCL10, and RELB while expression of the NF-κB target gene IRF4 is suppressed. MCEIn Vivo:MLT-231 (10-100mg/kg; p.o.; bid schedule for 2 weeks) displays in vivo efficacy in the ABC-DLBCL xenograft model. MLT-231 (1mg/kg; i.v.; BALB/c mice) treatment shows the CL, t 1/2, and V ss are 11 mL/min/kg, 1.9 hours, and 1.5 L/kg, respectively.Biological Activity:MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC 50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC 50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse