ML-264

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ML-264

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1550008-55-3

包装与价格：

包装	价格(元)
5mg	询价
10mg	询价
25mg	询价

化学性质

Physical Appearance	A crystalline solid
Storage	Store at -20°C
M.Wt	384.9
Cas No.	1550008-55-3
Formula	C₁₇H₂₁ClN₂O₄S
Solubility	≤10mg/ml in DMSO;15mg/ml in dimethyl formamide
Chemical Name	(2E)-3-(3-chlorophenyl)-N-[2-[methyl(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)amino]-2-oxoethyl]-2-propenamide
Canonical SMILES	ClC1=CC=CC(/C=C/C(NCC(N(C)C2CCS(CC2)(=O)=O)=O)=O)=C1
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

ML264, a potent and selective inhibitor of kruppel-like factor 5 (KLF5), inhibits the growth of colorectal cancer. ML264 is chemically stable, unreactive with glutathione, has suitable aqueous solubility, is highly stable to mouse, rat, and human hepatic microsomes, making it a good candidate for in vivo anticancer studies [1].

ML264 inhibits the MAPK pathway by reducing EGR1 and KLF5 levels. KLF5 is a zinc finger-containing transcription factor which is highly expressed in rapidly dividing intestinal epithelial cells. KLF5 binds to GC-rich sequences in promoters of numerous genes, such as cyclin D1, cyclin B1/Cdc2, and integrin-linked kinase. KLF5 mediates the transforming effects of oncogenic H-Ras and plays an important role in regulating colon cancer pathogenesis [1].

In vitro: In a cell-based assay for proliferation of DLD-1 cells, the IC50 of ML264 was 29 nM. In a cell-based luciferase assay, the IC50 of ML264 was 81 nM. ML264 showed no cytotoxicity in the IEC-6 control cell line with an IC50 of >50 μM. The IC50 of ML264 was 560 nM, 130 nM and 130 nM in HCT116, HT29 and SW620, respectively. ML264 significantly reduced KLF5 expression. ML264 didn’t inhibit kinases associated with the KLF5 pathway. ML264 induced death of most colon cancer cell lines, with cytotoxicity toward several other tumor cell lines as well [1].

In vivo: In an established xenograft mouse model of colon cancer, ML264 efficiently inhibited growth of the tumor within five days treatment. This effect was caused by a significant reduction in proliferation and that ML264 potently inhibited the expression of KLF5 and EGR1, a transcriptional activator of KLF5 and EGR1, a transcriptional activator of KLF5 [2].

References:
[1]. Bialkowska A, Crisp M, Madoux F, et al. ML264: An Antitumor Agent that Potently and Selectively Inhibits Krüppel-like Factor Five (KLF5) Expression: A Probe for Studying Colon Cancer Development and Progression[J]. 2013.
[2]. de Sabando A R, Wang C, He Y, et al. ML264, A Novel Small-Molecule Compound That Potently Inhibits Growth of Colorectal Cancer[J]. Molecular cancer therapeutics, 2016, 15(1): 72-83.