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].

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^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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, t_1/2, and V_ss 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, t_1/2, and V_ss 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 AUC_0-24, C_max 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 AUC_0-24, C_max and F are 547 nM/h, 46 nM, and 61%, respectively.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

469.85

C₁₉H₁₉ClF₃N₇O₂

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 110 mg/mL (234.12 mM; Need ultrasonic)

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 6 mg/mL (12.77 mM); Clear solution

  此方案可获得 ≥ 6 mg/mL (12.77 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 60.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 5.5 mg/mL (11.71 mM); Clear solution

  此方案可获得 ≥ 5.5 mg/mL (11.71 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 55.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.