MLT-231|西域试剂

MLT-231,99.55%

产品编号：Bellancom-131902| 分子式：C₁₉H₁₉ClF₃N₇O₂| 分子量：469.85

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	包装	价格	库存与货期	购买量	操作
Bellancom-131902		￥5800.00	杭州北京（现货）
Bellancom-131902		￥9500.00	杭州北京（现货）

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MLT-231

产品介绍

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。

生物活性

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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	OCI-Ly3 cells
Concentration:	50-5000 nM
Incubation Time:	24 hours
Result:	NF-κB target gene IRF4 was suppressed.

体内研究
(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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Scid-beige mice (OCI-Ly10 ABC-DLBCL type xenograft model)
Dosage:	10, 30, and 100 mg/kg
Administration:	P.o.; bid schedule for 2 weeks
Result:	Led to tumor stasis, while being well tolerated.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Scid-beige mice (OCI-Ly10 ABC-DLBCL type xenograft model)
Dosage:	10, 30, and 100 mg/kg
Administration:	P.o.; bid schedule for 2 weeks
Result:	Led to tumor stasis, while being well tolerated.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Scid-beige mice (OCI-Ly10 ABC-DLBCL type xenograft model)
Dosage:	10, 30, and 100 mg/kg
Administration:	P.o.; bid schedule for 2 weeks
Result:	Led to tumor stasis, while being well tolerated.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1283 mL	10.6417 mL	21.2834 mL
5 mM	0.4257 mL	2.1283 mL	4.2567 mL
10 mM	0.2128 mL	1.0642 mL	2.1283 mL

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。