2840558-83-8

Name	Benzamide, 3-[(2'-methoxy[3,4'-bipyridin]-2-yl)oxy]-N-methyl-5-(trifluoromethoxy)-
CAS	2840558-83-8
Molecular Formula	C20H16F3N3O4
Molecular Weight	419.35
MOL File	2840558-83-8.mol

Synonyms

Aurora Kinases-IN-3 Benzamide, 3-[(2'-methoxy[3,4'-bipyridin]-2-yl)oxy]-N-methyl-5-(trifluoromethoxy)-

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Chemical Properties

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

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.

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), C_max 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

Supplier

Shanghai Beckham Medical Technology Co., Ltd

Telephone 13816613772

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList16976/0_EN.htm

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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