| 货号 | 21531-25mg |
| 描述 | ACY-1215 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 5 nM).1 It is at least 10-fold less active against other HDACs in enzymatic assays. ACY-1215 shows synergistic activity with the proteasome inhibitor bortezomib (Item No. 10008822) against multiple myeloma (MM) cells, inducing protracted endoplasmic reticulum stress and apoptosis.1,2 ACY-1215 combined with proteasome inhibitors suppresses tumor growth and increases survival in mice with MM and mantle cell lymphoma xenografts.2,1,3 A multicenter phase I trial examining ACY-1215 combined with the E3 ligase inhibitor lenalidomide (Item No. 14643) and dexamethasone (Item No. 11015) in multiple myeloma found inhibition of HDAC6 in vivo.4 ACY-1215 also diminishes liver cyst development and fibrosis in a rat model of polycystic liver disease.5 |
| 别名 | ACY-63;Ricolinostat;Rocilinostat; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Santo, L.,Hideshima, T.,Kung, A.L., et al. Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. Blood 119(11), 2579-2589 (2012). 2.Amengual, J.E.,Johannet, P.,Lombardo, M., et al. Dual targeting of protein degradation pathways with the selective HDAC6 inhibitor ACY-1215 and bortezomib is synergistic in lymphoma. Clin. Cancer Res. 21(20), 4663-4675 (2015). 3.Dasmahapatra, G.P.,Patel, H.,Friedberg, J., et al. In vitro and in vivo interactions between the HDAC6 inhibitor ricolinostat (ACY1215) and the irreversible proteasome inhibitor carfilzomib in non-Hodgkin lymphoma cells. Mol. Cancer Ther. 13(12), 2886-2897 (2014). 4.Yee, A.J.,Bensinger, W.I.,Supko, J.G., et al. Ricolinostat plus lenalidomide, and dexamethasone in relapsed or refractory multiple myeloma: A multicentre phase 1b trial. Lancet Oncol. 17(11), 1569-1578 (2016). 5.Gradilone, S.A.,Habringer, S.,Masyuk, T.V., et al. HDAC6 is overexpressed in cystic cholangiocytes and its inhibition reduces cystogenesis. Am. J. Pathol. 184(3), 600-608 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 433.5 |
| 分子式 | C24H27N5O3 |
| CAS号 | 1316214-52-4 |
| 稳定性 | ≥ 2 years |
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