WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 200115
Description: AEZS-112, also known as ZEN012, is an orally active small mol. anti-cancer drug which inhibits the polymn. of tubulin at low micromolar concns. AEZS 112 dose-dependently increased non-vital hypodiploid cells and the cytotoxic effect was least pronounced in G2 phase of the cell cycle, indicating cell death during mitosis, as detd. by FACS anal. AEZS 112 showed anti-tumor activity in human ovarian and endometrial cancer cell lines at low micromolar concns., which could not be abrogated by caspase inhibition and is therefore a good candidate for in vivo studies in these tumors.
MedKoo Cat#: 200115
Chemical Formula: C25H23N3O2
Exact Mass: 397.17903
Molecular Weight: 397.46902
Elemental Analysis: C, 75.54; H, 5.83; N, 10.57; O, 8.05
Synonym: ZEN012; ZEN 012; ZEN-012; AEZS112; AEZS 112; AEZS-112.
IUPAC/Chemical Name: 9-Acridinyl[4-(3-methoxyphenyl)-1-piperazinyl]methanone
InChi Key: YTECZQLINBWBIQ-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H23N3O2/c1-30-19-8-6-7-18(17-19)27-13-15-28(16-14-27)25(29)24-20-9-2-4-11-22(20)26-23-12-5-3-10-21(23)24/h2-12,17H,13-16H2,1H3
SMILES Code: O=C(C1=C(C=CC=C2)C2=NC3=CC=CC=C31)N4CCN(C5=CC=CC(OC)=C5)CC4
AEZS-112 is currently developed by Ã†terna Zentaris Inc. AEZS-112 is the first anticancer drug in development involving two mechanisms of action, tubulin and topoisomerase II inhibition. AEZS-112 expresses different modes of action such as, pro-apoptotic and anti-angiogenic properties.
Mode of action studies revealed that the compound AEZS-112 inhibits the polymerization of ÃŸ-tubulin in low micromolar concentrations. Competition studies suggest that AEZS-112 interacts with the same binding site on microtubules as colchicine. AEZS-112 destroys the mitotic spindles of the cancer cells, arrests the cancer cells in G2/M phase at low concentrations, mediates DNA fragmentation via inhibition of topoisomerase II and induces apoptosis via various mechanisms. See Ã†terna Zentaris Inc's website.
1: Kwok CW, Treeck O, Buchholz S, Seitz S, Ortmann O, Engel JB. Receptors for luteinizing hormone-releasing hormone (GnRH) as therapeutic targets in triple negative breast cancers (TNBC). Target Oncol. 2014 Oct 9. [Epub ahead of print] PubMed PMID: 25293576.
2: Engel JB, Schönhals T, Weidler C, Häusler S, Krockenberger M, Rieger L, Dietl J, Wischhusen J, Honig A. Tubulin inhibitor AEZS 112 inhibits the growth of experimental human ovarian and endometrial cancers irrespective of caspase inhibition. Oncol Rep. 2009 Aug;22(2):361-7. PubMed PMID: 19578778.