产品
编 号：F756300
分子式：C20H16F3N3O4
分子量：419.35
分子式：C20H16F3N3O4
分子量：419.35
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 2840558-83-8
产品详情
生物活性：
Aurora Kinases-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.
体内研究：
Aurora Kinases-IN-3 (Compound 15a) (50 mg/kg; oral; twice a day for 7 days) 抑制小鼠肺部肿瘤的生长。Animal Model:Female BALB/c nude mice bearing a xenograft of the human lung cancer cell line NCI–H23
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
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.
体外研究：
Aurora Kinases-IN-3 (Compound 15a) (40 nM; 6 h) disrupts localization of AURKB, MKLP1, and PLK at the spindle midzone to prevent spindle midzone microtubule assembly in RPE-MYCBCL2 cells. Aurora Kinases-IN-3 disrupts the localization of AURKB as early as anaphase, producing downstream consequences that blocked cytokinesis.Aurora Kinases-IN-3 (1-10 μM; 3 days) shows wide spectrum of growth suppression in human cancer cell lines.
Aurora Kinases-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.
体内研究：
Aurora Kinases-IN-3 (Compound 15a) (50 mg/kg; oral; twice a day for 7 days) 抑制小鼠肺部肿瘤的生长。Animal Model:Female BALB/c nude mice bearing a xenograft of the human lung cancer cell line NCI–H23
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
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.
体外研究：
Aurora Kinases-IN-3 (Compound 15a) (40 nM; 6 h) disrupts localization of AURKB, MKLP1, and PLK at the spindle midzone to prevent spindle midzone microtubule assembly in RPE-MYCBCL2 cells. Aurora Kinases-IN-3 disrupts the localization of AURKB as early as anaphase, producing downstream consequences that blocked cytokinesis.Aurora Kinases-IN-3 (1-10 μM; 3 days) shows wide spectrum of growth suppression in human cancer cell lines.
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