Tacedinaline (N-acetyldinaline) is a novel oral compound with a wide spectrum of antitumor activity in preclinical models. The mechanism of action may involve inhibition of histone deacetylation and cell cycle arrest. Tacedinaline (N-acetyldinaline) is combined with antineoplastic agents commonly used in non-small cell lung cancer cell line management, a marked synergism of action (R=1.8, R=1.5) is observed between Tacedinaline (N-acetyldinaline) (40 μM) and gemcitabine (0.01 μM) at 48 and 72 h of treatment. Tacedinaline (N-acetyldinaline) inhibits mitogen-stimulated blood lymphocyte proliferation with an IC50 value of 3 μM.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 5 mg | In stock | $ 63 | |
| 10 mg | In stock | $ 113 | |
| 20 mg | In stock | $ 178 | |
| 50 mg | In stock | $ 376 | |
| 100 mg | In stock | $ 597 |
| Description | Tacedinaline (N-acetyldinaline) is a novel oral compound with a wide spectrum of antitumor activity in preclinical models. The mechanism of action may involve inhibition of histone deacetylation and cell cycle arrest. Tacedinaline (N-acetyldinaline) is combined with antineoplastic agents commonly used in non-small cell lung cancer cell line management, a marked synergism of action (R=1.8, R=1.5) is observed between Tacedinaline (N-acetyldinaline) (40 μM) and gemcitabine (0.01 μM) at 48 and 72 h of treatment. Tacedinaline (N-acetyldinaline) inhibits mitogen-stimulated blood lymphocyte proliferation with an IC50 value of 3 μM. |
| Targets&IC50 | HDAC1: 0.9 μM, HDAC3: 1.2 μM, HDAC2: 0.9 μM |
| In vitro | LNCaP cell lines are maintained in RPMI 1640 medium containing 10% fetal bovine serum, 1% penicillin and streptomycin, as the complete culture medium. Cells (2×104) are seeded in 24-well plates and incubated in a 5% CO2 incubator at 37 °C for 1 day. Cultures are treated with CI-994, alone and in combination on day 2 and 4. Cells are washed on day 2 and 4 and media are changed. Mitochondrial metabolism is measured as a marker for cell growth by adding 100 μL/well MTT (5 mg/mL in medium) with 2 hours incubation at 37 °C on Day 6. Crystals formed are dissolved in 500 μL of DMSO. The absorbance is determined using a microplate reader at 560 nm. The absorbance data are converted into cell proliferation percentage. Each assay is performed in triplicate. (Only for Reference) |
| Synonyms | CI994, PD-123654, Acetyldinaline, Goe-5549, N-acetyldinaline |
| CAS No. | 112522-64-2 |
| Chemical Formula | C15H15N3O2 |
| Molecular Weight | 269.304 |
| Solubility | DMSO: 26.9 mg/mL (100 mM) |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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