CI-994 4-acetylamino-n-(2'-aminophenyl)benzamide;Benzamide, 4-(acetylamino)-N-(2-aminophenyl)-;acetyldinaline;Tacedinaline;CI 994;N-Acetyldinaline;4-AcetaMido-N-(2-aMinophenyl)benzaMide;Cl-994(Tacedinalin,N- 112522-64-2
CI-994 (Tacedinaline) is an anti-cancer drug which inhibits HDAC1 with IC50 of 0.57 μM and causes G1 cell cycle arrest.
IC50 Value: 0.57 uM (For HDAC1,MTT assay)
Target: HDAC1
in vitro: Different CI-994 concentrations were tested, ranging from 0.01 to 160 microM at 24, 48, and 72 h of treatment inA-549 (adenocarcinoma) and LX-1 (squamous cell carcinoma) ,with MTT assay. A concentration-dependent cell survival inhibition was observed, with an IC50 at 80 microM. The effect of CI-994, as demonstrated by recovery experiments, was cytostatic and seemed to be superimposable in both cell lines. Cytofluorimetric analysis to assess cell cycle perturbation and apoptosis was performed after 24 h of treatment, indicating a cell block with concomitant increase at G0/G1 phase, a reduction at S phase level at 20, 40, 80, and 160 microM, and apoptosis at the higher concentration (160 microM) [1].
in vivo: CI-994 had the same spectrum of activity in vivo as dinaline. It also behaved similarly in schedule comparison/toxicity trials. Prolonged administration with lower drug doses was more effective than short-term therapy at higher individual doses. If doses were kept between 40 and 60 mg/kg/injection, prolonged administration (> 50 days) was tolerated with no gross toxicity. Doses > or = 90 mg/kg/injection caused lethality after 4-5 days of administration[2]. IC994 is currently in Phase I/II clinical trials, combining with gemcitabine[3].
Clinical trail: CI-994 is in Phase III clinical trial in patients with Lung Cancer.
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