CI-994 (Tacedinaline)是抗癌化合物,能抑制HDAC1,IC50为0.57 μM,能促使细胞周期停滞于G1期。
CI-994 (Tacedinaline) is an anti-cancer drug which inhibits HDAC1 with IC50 of 0.57 μM and causes G1 cell cycle arrest[1]. CI-994 (< 160 mM) shows cytostatic effect with concomitant increase at G0/G1 phase, a reduction at S phase level and increased apoptosis in A-549 and LX-1 cells.
30% PEG400+0.5% Tween80+5% propylene glycol
2.5 μM
535 mg/kg通过口服给药
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
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。
[1] Methot JL, et al. Bioorg Med Chem Lett, 2008, 18(3), 973-978.
[2] Beckers, Thomas., et al., 2007. Distinct pharmacological properties of second generation HDAC inhibitors with the benzamide or hydroxamate head group. International journal of cancer. Journal international du cancer. 121(5): 1138-48.
[3] Kraker, Alan J., et al., 2003. Modulation of histone acetylation by [4-(acetylamino)-N-(2-amino-phenyl) benzamide] in HCT-8 colon carcinoma. Molecular cancer therapeutics. 2(4): 401-8.
分子式 C15H15N3O2 |
分子量 269.3 |
CAS号 112522-64-2 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 100 mM |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00005624 | Multiple Myeloma | Drug: CI-994 | H. Lee Moffitt Cancer Center and Research Institute|National Cancer Institute (NCI)|Parke-Davis | Phase 2 | 1997-08-01 | 2012-09-21 |
NCT00005093 | Lung Cancer | Drug: gemcitabine hydrochloride|Drug: tacedinaline | Pfizer | Phase 3 | 1999-12-01 | 2012-08-08 |
NCT00004861 | Pancreatic Cancer | Drug: gemcitabine hydrochloride|Drug: tacedinaline | Pfizer | Phase 2 | 1999-10-01 | 2012-08-08 |
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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