| Identification | Back Directory | [Name]
Benzamide, 3-[(2'-methoxy[3,4'-bipyridin]-2-yl)oxy]-N-methyl-5-(trifluoromethoxy)- | [CAS]
2840558-83-8 | [Synonyms]
Aurora Kinases-IN-3
Benzamide, 3-[(2'-methoxy[3,4'-bipyridin]-2-yl)oxy]-N-methyl-5-(trifluoromethoxy)- | [Molecular Formula]
C20H16F3N3O4 | [MOL File]
2840558-83-8.mol | [Molecular Weight]
419.35 |
| Chemical Properties | Back Directory | [Boiling point ]
483.9±45.0 °C(Predicted) | [density ]
1.324±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
14.32±0.46(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Aurora kinase-IN-3 (Compound 15a) is an orally active AURKB inhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB, rather than inhibiting its phosphorylation of H3 at Ser10[1]. | [in vivo]
Aurora kinase-IN-3 (Compound 15a) (50 mg/kg; oral; twice a day for 7 days) suppresses the growth of lung tumors in mice[1]. | Animal Model: | Female BALB/c nude mice bearing a xenograft of the human lung cancer cell line NCI–H23[1] | | Dosage: | 50 mg/kg | | Administration: | Oral gavage, twice a day for 7 days | | Result: | Elicited a mitotic arrest and induced cell death by apoptosis. Effectively suppressed the growth of the tumor and reduced the cellularity of tumor tissue.
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| Animal Model: | Female BAL B/c nude mice[1] | | Dosage: | 50 mg/kg | | Administration: | Oral administration (Pharmacokinetic Analysis) | | Result: | After oral delivery in PEG300, achieved adequate plasma exposure, the mean value of dose-normalized area under the dose-response curve (AUC) was 0.35 x h/(mg/kg), Cmax was 6.9 μM. Was barely absorbed after oral gavage in the hydrophilic hydroxypropyl methylcellulose (HPMC) formulation. |
| [References]
[1] Lv G, et al. 2-Phenoxy-3, 4'-bipyridine derivatives inhibit AURKB-dependent mitotic processes by disrupting its localization. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114904. DOI:10.1016/j.ejmech.2022.114904 |
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