Aurora Kinases-IN-3 (Compound 15a) 是一种具有口服活性的AURKB抑制剂，通过破坏 AURKB 的有丝分裂定位，而不是抑制其在 Ser10 位点 H3 的磷酸化，从而诱导 AURKB 抑制活性。
| 生物活性 | Aurora Kinases-IN-3 (Compound 15a) is an orally activeAURKBinhibitor that elicits an AURKB-suppressive activity by disrupting the mitotic localization of AURKB, rather than inhibiting its phosphorylation of H3 at Ser10[1]. |
| IC50& Target | |
体外研究
(In Vitro) | 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-MYCBCL2cells. Aurora Kinases-IN-3 disrupts the localization of AURKB as early as anaphase, producing downstream consequences that blocked cytokinesis[1].
Aurora Kinases-IN-3 (1-10 μM; 3 days) shows wide spectrum of growth suppression in human cancer cell lines[1].
Cell Viability Assay[1] | Cell Line: | NCI–H23, A549, HCT116, SW480, MDA-MB-231, HeLa and NCI-87 cells | | Concentration: | 1, 2.5, 5, or 10 μM | | Incubation Time: | 3 days | | Result: | Exhibited the EC50values of about 10 nM in most cell lines. |
|
体内研究
(In Vivo) | 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[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), Cmaxwas 6.9 μM. Was barely absorbed after oral gavage in the hydrophilic hydroxypropyl methylcellulose (HPMC) formulation. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com