M-525 ( M525 )

产品货号. M13475 CAS No. 2173582-08-4

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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产品名称

M-525
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

M-525 是一种首创、高效、不可逆的 menin-MLL 相互作用小分子抑制剂，在 FP 测定中结合 IC50 为 3.3 nM。
产品描述

M-525 is a first-in-class, highly potent, irreversible small-molecule inhibitor of the menin-MLL interaction with binding IC50 of 3.3 nM in FP assays; inhibits MV4;11 (MLL fusion) and HL60 (No MLL fusion) cell growth with IC50 of 2.7 and 2,000 nM, respectively; significantly down-regulates the expression of MEIS1, HOXA9 and HOXA11 genes in a dosedependent anner at ow nanomolar concentrations, also effectively suppresses the expression of MEIS1 and HOX genes in the MOLM-13 cell line at 3 nM.
体外实验

M-525 achieves an IC50 of 3 nM in the MV4;11 cell line and has an IC50 of 2 μM in the HL-60 cell line. M-525 (3-300 nM; 24 h) is potent and effective in suppressing the expression of MEIS1 and HOX genes in MV4;11 cells carrying the MLL-AF4 fusion and in MOLM-13 cells carrying the MLL-AF9 fusion. It demonstrates high cellular specificity over non-MLL leukemia cells.
体内实验

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同义词

M525
通路

Chromatin/Epigenetic
靶点

HMTase
受体

HMTase
研究领域

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适应症

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CAS Number

2173582-08-4
分子量

734.932
分子式

C39H51FN6O5S
纯度

>98% (HPLC)
溶解度

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SMILES

O=C(OC)N[C@@H]1[C@@H]([C@](C2=CC=CC(F)=C2)(C3CCN(CC4CN(C5=CC=C(S(=O)(C6CN(C(/C=C/CN(C)C)=O)C6)=O)C=C5)C4)CC3)O)CCC1
化学全称

methyl ((1S,2R)-2-((S)-cyano(1-((1-(4-((1-((E)-4-(dimethylamino)but-2-enoyl)azetidin-3-yl)sulfonyl)phenyl)azetidin-3-yl)methyl)piperidin-4-yl)(3-fluorophenyl)methyl)cyclopentyl)carbamate