Information
Entinostat (MS-275, SNDX-275) strongly inhibitsHDAC1andHDAC3withIC50of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat inducesautophagyandapoptosis. Phase 3.
In vitro
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
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.
Cell Data
cell lines：
Concentrations：~ 10 μM
Incubation Time：3 days
Powder Purity:≥97%
