CI-994 CAS NO.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.