Rocilinostat (ACY-1215),1316214-52-4

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YZ剂描述：

产品名称：Rocilinostat (ACY-1215)

产品别名：2-(二苯基氨基)-n-[7-(羟基氨基)-7-氧代庚基]-5-嘧啶羧酰胺

英文别名：Ricolinostat;ACY1215;ACY 1215

靶点：HDAC6 ,HDAC2 ,HDAC3 ,HDAC1 ,HDAC8

CAS：1316214-52-4

纯度：＞98%

外观：白色粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Rocilinostat (ACY-1215)是一种选择性HDAC6YZ剂，无细胞试验中IC50为5 nM，作用于HDAC6比作用于HDAC1/2/3(I型HDACs)选择性高10倍以上，对HDAC8具有微弱的作用活性，对HDAC4/5/7/9/11， Sirtuin1和Sirtuin2具有Z小的作用活性。

溶解性：DMSO : 80 mg/mL (184.5 mM)

体外研究：

ACY-1215 is a hydroxamic acid derivative. ACY-1215 is 12-, 10-, and 11-fold less active against HDAC1, HDAC2, and HDAC3 (class I HDACs), respectively. ACY-1215 has minimal activity (IC50 > 1μM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2, and has slight activity against HDAC8 (IC50 = 0.1μM). The IC50 values for ACY-1215 for T-cell toxicity is 2.5μM. ACY-1215 overcomes tumor cell growth and survival conferred by BMSCs and cytokines in the BM milieu. ACY-1215 in combination with bortezomib induces synergistic anti-MM activity. ACY-1215 induces potent acetylation of α-tubulin at very low doses and triggers acetylation of lysine on histone H3 and histone H4 only at higher doses, confirming its specific inhibitory effect on HDAC6 activity.

体内研究：ACY-1215 in combination with bortezomib triggered more significant anti-MM activity than either agent alone in suppressing tumor growth and prolonging survival in both plasmacytoma model and disseminated MM model without significant adverse effects. ACY-1215 is readily absorbed by tumor tissue. Moreover, the drug does not accumulate in tumor tissue, as evidenced by the parallel decline of acetylated α-tubulin in blood cells and tumor tissue by 24 hours after dose.

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