Entinostat (MS-275, SNDX-275)

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Entinostat (MS-275, SNDX-275)CAS号： 209783-80-2分子式： C21H20N4O3分子量： 376.41描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献

产品描述
描述

Entinostat (MS-275)强烈抑制HDAC1和HDAC3，无细胞试验中IC50分别为0.51 μM和1.7 μM，抑制作用强于HDACs 4， 6， 8，和10。
纯度
＞98%
储存/保存方法
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
基本信息
别名
恩替诺特；MS-275；SNDX-275
外观
白色粉末
可溶性/溶解性
DMSO : 37.6 mg/mL (100 mM)
生物活性
靶点
HDAC1 ,HDAC3
In vitro(体外研究)
MS-275 shows inhibitory to HDACs by 2′-amino group. MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. MS-275 could reduce S-phase cells and induce G1-phase cells in A2780 cell. MS-275 inhibits the proliferation of human tumor cell lines including A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 with IC50 from 41.5 nM to 4.71 μM, which due to HAD-inhibition. MS-275 is not sensitive to other HDACs (4, 6, 8 and 10) with IC50 about/above 100 μM. MS-275 shows great inhibition to human leukemia and lymphoma cells, including U937, HL-60, K562, and Jurkat. MS-275 also decreases expression of cyclin D1 and the antiapoptotic proteins Mcl-1 and XIAP.
In vivo(体内研究)
MS-275 exhibits great antitumor activity against human tumor xenografts except HCT-15 at 49 mg/kg. MS-275 demonstrates promising therapeutic potential in both solid and hematologic malignancies, as well as regulation of physiologic and aberrant gene expression. MS-275, combination with IL-2, has great antitumor activity to renal cell carcinoma xenograft model, which due to decreased T regulatory cells and increased splenocytes.
参考文献
参考文献

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[3] Rosato RR, et al. Cancer Res, 2003, 63(13), 3637-3645.

[4] Zhang ZY, et al. Neurosci, 2010, 169, 370-377.

[5] Kato Y, Clin Cancer Res, 2007, 13(15), 4538-4546.

[6] Wegener D, et al. Chem Biol, 2003, 10(1), 61-68.

分子结构图

Entinostat (MS-275, SNDX-275)