Cas No.: | 112522-64-2 |
Chemical Name: | Tacedinaline |
Synonyms: | 4-Acetamido-N-(2-aminophenyl)benzamide;Tacedinaline;CI-994;CI994 (Tacedinaline);4-ACETYLAMINO-N-(2'-AMINOPHENYL)BENZAMIDE;CI 994;CI-994 (Acetyldinaline,Goe 5549,Gö 5549,PD 123654,Tacedinaline);Acetyldinaline;Goe 5549;N-acetyldinaline;PD 123654;Tacedinalina;4-Acetylamino-N-(2′-aminophenyl)benzamide;CI-994 (Acetyldinaline,PD123654);Cl-994(Tacedinalin,N-Acetyldinalin);CI994, >=99%;Tacedinaline [USAN:INN];CI994;Tacedinalina [INN-Spanish];4-(Acetylamino)-N-(2-aminophenyl)benzamide;C.I. 994;UMF554N5FG;C15H15N3O2;Benzamide, 4-(acetylamino)-N-(2-aminophenyl)-;Tacedinaline (USAN/INN);4-acetamido-n-(2-aminophenyl)benza;ci994-tacedinaline;MLS006010120;GTPL8367;ZIN |
SMILES: | O=C(C1C([H])=C([H])C(=C([H])C=1[H])N([H])C(C([H])([H])[H])=O)N([H])C1=C([H])C([H])=C([H])C([H])=C1N([H])[H] |
Formula: | C15H15N3O2 |
M.Wt: | 269.2985 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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. |
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]. |
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]. |