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MI-538

    
≥98%

MI-538

源葉(MedMol)
S84091 一鍵復制產(chǎn)品信息
1857417-10-7
C27H25F3N8OS
566.6006
貨號 規(guī)格 價格 上海 北京 武漢 南京 購買數(shù)量
S84091-1mg
≥98% ¥1100.00 貨期:2-3天 - - -
S84091-5mg
≥98% ¥2400.00 貨期:2-3天 - - -
S84091-10mg
≥98% ¥4200.00 貨期:2-3天 - - -
產(chǎn)品介紹 參考文獻 質(zhì)檢證書(COA) 摩爾濃度計算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM

產(chǎn)品描述: MI-538 is an inhibitor of the interaction between menin and MLL fusion proteins with an IC50 of 21 nM
靶點: IC50 : 21 nM (menin and MLL interaction); Kd: 6.5 nM (menin);EpigeneticReaderDomain;?HistoneMethyltransferase
體外研究: MI-538 inhibits the proliferation of MLL leukemia cells with a GI50 of 83 nM. MI-538 shows no effect (up to 6 μM) on growth of the control cell lines HL-60 and HM-2, which do not harbor MLL translocations, demonstrating good selectivity toward MLL fusion protein transformed cells. MI-538 binds to menin with low nanomolar affinity (Kd=6.5 nM). Its potent cellular activity originates from the improved binding affinity to menin and possibly increased cell membrane permeability. Treatment with MI-538 results in strong down regulation of expression of Hoxa9 and Meis1 genes. About 100 nM 27 was sufficient to reduce by ~50% Hoxa9 expression in MLL-AF9 cells, and even more pronounced effect was seen on Meis1 expression
體內(nèi)研究: Treatment with MI-538 results in a pronounced, about 80%, reduction in the MV4;11 tumor volume, without causing substantial signs of toxicity reflected by less than 10% reduction of the body weight. MI-538 demonstrates markedly improved exposure (area under the curve, AUC, values), Cmax (maximum compound concentration) in the blood plasma, and the lowest value of clearance. The half-life of MI-538 is about 1.6 h. MI-538 has also high oral bioavailability (~50%)
參考文獻: 1. Borkin D, et al. Property Focused Structure-Based Optimization of Small Molecule Inhibitors of the Protein-Protein Interaction between Menin and Mixed Lineage Leukemia (MLL). J Med Chem. 2016 Feb 11;59(3):892-913.
溶解性: soluble  in  DMSO
保存條件: -20℃
配置溶液濃度參考:
1mg 5mg 10mg
1 mM 1.765 ml 8.825 ml 17.649 ml
5 mM 0.353 ml 1.765 ml 3.53 ml
10 mM 0.176 ml 0.882 ml 1.765 ml
50 mM 0.035 ml 0.176 ml 0.353 ml
注意: 部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。

參考文獻

質(zhì)檢證書(COA)

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批號:JS298415 貨號:S20001-25g
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摩爾濃度計算器

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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