产品
编 号:F639121
分子式:C21H13Cl2N3O2S
分子量:442.32
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规格
价格
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5mg
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10mg
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25mg
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50mg
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产品详情
生物活性:
AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, which can cause mitotic delay and arrest cells in a prometaphase, reflecting by the biomarker histone H3Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM.

体内研究:
AAPK-25 enhances survival rate in the BALB/c nude mice tumor xenograft model.

体外研究:
AAPK-25 inhibits HCT-116, Calu6, A549 and MCF-7 cells growth with IC50s of 0.4, 5.3, 11.6, and 2.3 μM, respectively.AAPK-25 induces apoptosis as a dose-dependent manner in HCT-116 cell line.AAPK-25 has significantly increased histone H3Ser10 phosphorylation, indicating a markedly mitotic block.AAPK-25 is in notably inhibition of the mitotic spindle checkpoint, which is mainly mediated by cell cycle signaling and mitotic pathways.
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