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MLT-231 is a potent, highly selective allosteric MALT1 Inhibitor with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse[1]. | [in vivo]
MLT-231 (10-100 mg/kg; p.o.; bid schedule for 2 weeks) displays in vivo efficacy in the ABC-DLBCL xenograft model[1].
MLT-231 (1 mg/kg; i.v.; BALB/c mice) treatment shows the CL, t1/2, and Vss are 11 mL/min/kg, 1.9 hours, and 1.5 L/kg, respectively[1].
MLT-231 (1 mg/kg; i.v.; Sprague-Dawley rats) treatment shows the CL, t1/2, and Vss are 41 mL/min/kg, 3.2 hours, and 9.4 L/kg, respectively[1].
MLT-231 (3 mg/kg; p.o.; BALB/c mice) treatment shows the AUC0-24, Cmax and F are 3096 nM/h, 549 nM, and 99%, respectively[1].
MLT-231 (3 mg/kg; p.o.; Sprague-Dawley rats) treatment shows the AUC0-24, Cmax and F are 547 nM/h, 46 nM, and 61%, respectively. | Animal Model: | Scid-beige mice (OCI-Ly10 ABC-DLBCL type xenograft model)[1] | | Dosage: | 10, 30, and 100 mg/kg | | Administration: | P.o.; bid schedule for 2 weeks | | Result: | Led to tumor stasis, while being well tolerated.
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| [References]
[1] Pissot Soldermann C, et al. Discovery of Potent, Highly Selective, and In Vivo Efficacious, Allosteric MALT1 Inhibitors by Iterative Scaffold Morphing [published online ahead of print, 2020 Nov 30]. J Med Chem. 2020;10.1021/acs.jmedchem.0c01245. DOI:10.1021/acs.jmedchem.0c01245 |
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