Cat. No. Name Size Price Add Cart
KI3681CI99410 mg$120
CI99450 mg$460

Chemical Characteristic

Product NameCI994
SynonymsTacedinaline
CAS No.112522-64-2
Molecular Weight 269.3
FormulaC15H15N3O2
Chemical Name4-Acetylamino-N-(2'-aminophenyl)benzamide
SmilesC(=O)(c1ccc(cc1)NC(=O)C)Nc1c(cccc1)N
Chemical Structure

Biological activities

CI-994 (Tacedinaline) is an anti-cancer drug which inhibits HDAC1 with IC50 of 0.57 ?M and causes G1 cell cycle arrest, and CI-994 is in Phase III clinical trial in patients with Lung Cancer [1]. In vitro, CI-994 in combination with cytarabine (ara-C), daunorubicin and mitoxantrone, resulted in moderate synergism [2]. In vivo, higher dosages of CI-994 induced complete remissions. CI-994/ara-C was very active against BNML (Brown Norway rat acute myelocytic leukemia). The combinations of CI-994/daunorubicin and CI-994/mitoxantrone were also active against BNML [3].

References

[1] Richards D A, Boehm K A, Waterhouse D M, et al. Gemcitabine plus CI-994 offers no advantage over gemcitabine alone in the treatment of patients with advanced pancreatic cancer: results of a phase II randomized, double-blind, placebo-controlled, multicenter study. Annals of oncology.2006, 17(7): 1096-1102.
[2] Loprevite M, Tiseo M, Grossi F, et al. In vitro study of CI-994, a histone deacetylase inhibitor, in non-small cell lung cancer cell lines. Oncology Research Featuring Preclinical and Clinical Cancer Therapeutics, 2005, 15(1): 39-48.
[3] Thomas M, Clarhaut J, Tranoy-Opalinski I, et al. Synthesis and biological evaluation of glucuronide prodrugs of the histone deacetylase inhibitor CI-994 for application in selective cancer chemotherapy. Bioorganic & medicinal chemistry, 2008, 16(17): 8109-8116.

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