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MLT-231, a potent and highly selective allosteric MALT1 inhibitor, has an IC50 of 9 nM and specifically inhibits endogenous BCL10 cleavage with an IC50 of 160 nM. It exhibits antitumor activity in an ABC-DLBCL type xenograft mouse model[1].
MLT-231, a potent and highly selective allosteric MALT1 inhibitor, has an IC50 of 9 nM and specifically inhibits endogenous BCL10 cleavage with an IC50 of 160 nM. It exhibits antitumor activity in an ABC-DLBCL type xenograft mouse model[1].
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 5 mg | ¥ 4,665 | 待询 | |
| 10 mg | ¥ 7,662 | 待询 | |
| 25 mg | ¥ 13,800 | 待询 |
MLT-231 相关产品
| 产品描述 | MLT-231, a potent and highly selective allosteric MALT1 inhibitor, has an IC50 of 9 nM and specifically inhibits endogenous BCL10 cleavage with an IC50 of 160 nM. It exhibits antitumor activity in an ABC-DLBCL type xenograft mouse model[1]. |
| 体外活性 | 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]. |
| 体内活性 | 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. |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度信息 | DMSO: 110 mg/mL, Sonication is recommended. |
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 5 mg/mL, Sonication is recommeded. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 |
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