CI-994 (N-acetyldinaline) is a novel oral agent which inhibits HDAC1, with a wide spectrum of antitumor activity in preclinical models, in vitro and in vivo. CI-994 inhibits growth of LNCaP cell with IC50 of 7.4 μM. CI-994 inhibits growth of rat leukemia BCLO cells with IC50 of 2.5 μM. 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). CI-994 is currently in a phase III clinical trial in patients with lung cancer.
University of Otago. 2019.
Transcriptional effects of mood stabiliser drugs in a serotonergic cell line
CI-994 purchased from AbMole
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Source | AIDS Res Hum Retroviruses (2016). Figure 3. CI-994 |
| Method | Immunoblots | |
| Cell Lines | CD4+ T cells | |
| Concentrations | 0.57 μM | |
| Incubation Time | 24 h | |
| Results | Both vorinostat and panobinostat, but not tacedinaline, increased CDK9 T-loop phosphorylation in CCL19-treated cells compared to control cells. Vorinostat and panobinostat, but not tacedinaline, also increased histone H3 acetylation in CCl19-treated cells. |
| Molecular Weight | 269.3 |
| Formula | C15H15N3O2 |
| CAS Number | 112522-64-2 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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