Menin-MLL inhibitor MI-2,99.89%
产品编号:Bellancom-15222| CAS NO:1271738-62-5| 分子式:C18H25N5S2| 分子量:375.55
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Menin-MLL inhibitor MI-2
产品介绍 | Menin-MLL inhibitor MI-2 抑制 Menin-MLL 相互作用,IC50 为 446±28 nM。 | ||||||||||||||||
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生物活性 | Menin-MLL inhibitor MI-2 is a Menin-MLL interaction inhibitor with IC50 of 446±28 nM. | ||||||||||||||||
体外研究 |
Menin-MLL inhibitor MI-2 very effectively blocks proliferation of MLL-AF9 and MLL-ENL transduced BMC, with GI50 values of about 5 μM. Assessment of diverse hydrophobic groups at R1 led to the development of several compounds with IC50 values in the nanomolar range, including MI-2 (IC50= 446±28 nM) and MI-3 (IC50=648±25 nM).The dissociation constants measured for the menin-MLL inhibitors are at the nanomolar level, Kd=158 nM for MI-2. MI-2 can access the protein target and very effectively inhibit the menin-MLL-AF9 interaction in human cells. Furthermore, MI-2 shows only a small effect on the cell growth of E2A-HLF transduced BMC (GI50>50 μM), which may be due to inhibition of the menin interaction with wild-type MLL. Treatment with MI-2 results in GI50 values below 10 μM in MV4;11 (harboring MLL-AF4; GI50=9.5 μM), KOPN-8 (MLL-ENL; GI50=7.2 μM) and ML-2 (MLL-AF6; GI50=8.7 μM), and in MonoMac6 (MLL-AF9; GI50=18 μM). 西域 has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||||||
体内研究 | |||||||||||||||||
体内研究 | |||||||||||||||||
性状 | Solid | ||||||||||||||||
溶解性数据 |
In Vitro:
DMSO : 50 mg/mL (133.14 mM; Need ultrasonic) 配制储备液
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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
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运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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参考文献 |