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。

＞98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

恩替诺特；MS-275；SNDX-275

白色粉末

DMSO : 37.6 mg/mL (100 mM)

HDAC1 ,HDAC3

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.

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.

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