產(chǎn)品屬性:
產(chǎn)品名稱 | 規(guī)格 | CAS號 | 型號 |
AAPK-25 | 100mg 250mg 500mg | 2247919-28-2 | EY-Y0165081 |
Cas No.2247919-28-2
別名 N/A
化學名 N/A
分子式 C21H13Cl2N3O2S
分子量 442.32
溶解度 Soluble in DMSO
儲存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述:
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[1]. Kd: 23 nM (Aurora-A), 78 nM (Aurora-B), 289 nM (Aurora-C), 55 nM (PLK-1), 272 nM (PLK-2), 456 nM (PLK-3), 5.32 μM (ERK), 7.11 μM (PI3K), 8.02 μM (CDK)[1]
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[1].AAPK-25 induces apoptosis as a dose-dependent manner in HCT-116 cell line[1].AAPK-25 has significantly increased histone H3Ser10 phosphorylation, indicating a markedly mitotic block[1].AAPK-25 is in notably inhibition of the mitotic spindle checkpoint, which is mainly mediated by cell cycle signaling and mitotic pathways[1].
AAPK-25 enhances survival rate in the BALB/c nude mice tumor xenograft model[1].
[1]. Qi B, et al. Discovery of inhibitors of Aurora/PLK targets as anti-cancer agents. J Med Chem. 2019 Aug 5.
關鍵字: 2247919-28-2;C21H13Cl2N3O2S;AAPK-25;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學、分子生物學和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè),公司自成立以來,秉承""全心全意服務于科研工作者""的企業(yè)理念,立足生物科技領域,運用生物技術和科研試劑,發(fā)展現(xiàn)代生物科技,為各類大中小醫(yī)院及其它醫(yī)療機構、高等院校、科研院所、企事業(yè)單位提供優(yōu)質(zhì)的產(chǎn)品,服務生物科技領域的科學研究人員。
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