MLT-231 是一种高效、高选择性的变构 MALT1 抑制剂，IC₅₀ 为 9 nM。MLT-231 特异性地阻止内源性 BCL10 断裂，IC₅₀ 为 160 nM。MLT-23 在 ABC-DLBCL 型异种移植模型中具有抗肿瘤活性。

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.

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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. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis-tbl">

MLT-231 (10-100 mg/kg; p.o.; bid schedule for 2 weeks) displays in vivo efficacy in the ABC-DLBCL xenograft model.
MLT-231 (1 mg/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.
MLT-231 (1 mg/kg; i.v.; Sprague-Dawley rats) treatment shows the CL, t 1/2 , and V ss are 41 mL/min/kg, 3.2 hours, and 9.4 L/kg, respectively.
MLT-231 (3 mg/kg; p.o.; BALB/c mice) treatment shows the AUC 0-24 , C max and F are 3096 nM/h, 549 nM, and 99%, respectively.
MLT-231 (3 mg/kg; p.o.; Sprague-Dawley rats) treatment shows the AUC 0-24 , C max and F are 547 nM/h, 46 nM, and 61%, respectively. has not independently confirmed the accuracy of these methods.

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Powder -20°C 3 years；4°C 2 years

[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.

In Vitro: DMSO : 110 mg/mL (234.12 mM; Need ultrasonic)配制储备液