生物活性

MGCD0103 is a novel HDAC inhibitor, highly specific for classes I and IV HDACs, with IC50 of 0.15, 0.29 and 1.66 μM for HDAC 1, HDAC 2 and HDAC 3 respectively. MGCD0103 reveals most potent inhibitory activity against human HDAC1 and HDAC2 enzymes in vitro, and it does not inhibit class II HDACs. The inhibitory activity of MGCD0103 reaches the maximum plateau at 6 μM, and the maximal inhibitable enzyme pool affected by MGCD0103 is 75% of the total enzyme activity in HCT116 cells.

体外研究

体内研究

30% PEG400+0.5% Tween80+5% propylene glycol

激酶实验

细胞实验

0-60 μM

动物实验

80 mg/kg 口服处理

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Fournel M, et al. Mol Cancer Ther. 2008, 7(4), 759-768.
[2] Boumber Y, Younes A, Garcia-Manero G.,Mocetinostat (MGCD0103): a review of an isotype-specific histone deacetylase inhibitor.,Expert Opin Investig Drugs. 2011 Jun;20(6):823-9. Epub 2011 May 10.
[3] Siu LL, Pili R, Duran I, Messersmith WA, Chen EX, Sullivan R, MacLean M, King S, Brown S, Reid GK, Li Z, Kalita AM, Laille EJ, Besterman JM, Martell RE, Carducci MA. ,Phase I study of MGCD0103 given as a three-times-per-week oral dose in patients with advanced solid tumors.,J Clin Oncol. 2008 Apr 20;26(12):1940-7.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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