Tacedinaline,又称乙酰地那林,是I型HDAC选择性抑制剂,作用于HDAC 1/2/3/8的IC50分别为0.9、0.9、1.2和>20 μM,具有抗肿瘤活性。
参考文献
[1] Moradei OM, Mallais TC, Frechette S, et al. Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. J Med Chem. 2007 Nov 15;50(23):5543-6. doi: 10.1021/jm701079h(IF:6.054).
[2] Loprevite M, Tiseo M, Tiseo M, et, al. In vitro study of CI-994, a histone deacetylase inhibitor, in non-small cell lung cancer cell lines. Oncol Res. 2005;15(1):39-48. doi: 10.3727/096504005775082066(IF:4.634).
[3] Gediya LK, Belosay A, Khandelwal A, et, al. Improved synthesis of histone deacetylase inhibitors (HDIs) (MS-275 and CI-994) and inhibitory effects of HDIs alone or in combination with RAMBAs or retinoids on growth of human LNCaP prostate cancer cells and tumor xenografts. Bioorg Med Chem. 2008 Mar 15;16(6):3352-60. doi: 10.1016/j.bmc.2007.12.007(IF:2.802).
[4] LoRusso PM, Demchik L, Knight J, et, al. Preclinical antitumor activity of CI-994. Invest New Drugs. 1996;14(4):349-56. doi: 10.1007/BF00180810(IF:2.663).
-25~-15℃保存,有效期3年。