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Tacedinaline (CI994)
| Product Name | Tacedinaline (CI994) |
| Price: | Inquiry |
| Catalog No.: | CN00304 |
| CAS No.: | 112522-64-2 |
| Molecular Formula: | C15H15N3O2 |
| Molecular Weight: | 269.3 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | CC(=O)Nc1ccc(cc1)C(=O)Nc1ccccc1N |
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| Description | CI-994 (Tacedinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively. |
| Target | HD1:0.9 μM (IC50) HD2:0.9 μM (IC50) HD3:1.2 μM (IC50) |
| In Vitro | CI-994 (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. CI-994 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 CI-994 (40 μM) and gemcitabine (0.01 μM) at 48 and 72 h of treatment[2].CI-994 inhibits mitogen-stimulated blood lymphocyte proliferation with an IC50 value of 3 μM[4]. |
| In Vivo | CI-994 has activity against 8/8 solid tumors tested: pancreatic ductal adenocarcinoma #02 (4.7); pancreatic adenocarcinoma #03 (3.0; 1/6 cures); colon adenocarcinoma #38 (1.6); colon adenocarcinoma #51/A (1.1); mammary adenocarcinoma #25 (1.7); mammary adenocarcinoma #17/ADR (0.5); Dunning osteogenic sarcoma (4.0); and the human prostate carcinoma LNCaP (1.2). CI-994 is the acetylated metabolite of dinaline and has the same spectrum of activity in vivo as dinaline. It also behaves similarly in schedule comparison/toxicity trials[3]. CI-994 can effect lymphoid tissue in rats within 1 day of a single oral dose, that effects are generally reversible within 7 days[4]. |
| Animal Admin | Rats: To characterize the effects of CI-994 on lymphoid tissue, male rats are administered single oral doses at 0 (vehicle control), 10, 23, and 45 mg/kg and killed up to 7 days after dosing for evaluation of white blood cell differentials, bone marrow differentials, lymphoid tissue weights, and selected histopathology of lymphoid tissue[4]. |
| Density | 1.3±0.1 g/cm3 |
| Boiling Point | 450.6±30.0 °C at 760 mmHg |
| Flash Point | 226.3±24.6 °C |
| Exact Mass | 269.116425 |
| PSA | 84.22000 |
| LogP | 0.96 |
| Vapour Pressure | 0.0±1.1 mmHg at 25°C |