| Identification | Back Directory | [Name]
1H-1,2,3-Triazole-4-carboxamide, 1-[3-[(5-amino-2-chloro-4-fluoro-3-methylbenzoyl)amino]-4-(4-methyl-1-piperazinyl)phenyl]-N-[3-(4-morpholinyl)propyl]- | [CAS]
2250024-74-7 | [Synonyms]
DDO-2093
1H-1,2,3-Triazole-4-carboxamide, 1-[3-[(5-amino-2-chloro-4-fluoro-3-methylbenzoyl)amino]-4-(4-methyl-1-piperazinyl)phenyl]-N-[3-(4-morpholinyl)propyl]- | [Molecular Formula]
C29H37ClFN9O3 | [MOL File]
2250024-74-7.mol | [Molecular Weight]
614.11 |
| Hazard Information | Back Directory | [Uses]
DDO-2093 is a potent MLL1-WDR5 protein-protein interaction inhibitor (IC50=8.6 nM; Kd=11.6 nM) with antitumor activity. DDO-2093 selectively inhibits the catalytic activity of MLL complex[1]. | [in vivo]
DDO-2093 (20-80 mg/kg; i.p.; every other day for 21 days) significantly suppresses the tumor size and weight in a dose-dependent manner[1]. | Animal Model: | Female nude mice (MV4-11 human leukemia cancer xenografts)[1] | | Dosage: | 20 mg/kg, 40 mg/kg and 80 mg/kg | | Administration: | Intraperitoneal injection; every other day for 21 days | | Result: | Had the tumor volume growth inhibition (GI) values were calculated to be 13.7%, 37.6% and 63.9% with doses of 20 mg/kg, 40 mg/kg and 80 mg/kg, respectively.
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| [References]
[1] Chen W, et al. Discovery of a potent MLL1 and WDR5 protein-protein interaction inhibitor with in vivo antitumor activity [published online ahead of print, 2021 Jun 28]. Eur J Med Chem. 2021;223:113677. DOI:10.1016/j.ejmech.2021.113677 |
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