AAPK-25
规格
| Cas Number | 2247919-28-2 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 50mg 或 10mg 或 1mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : 50 mg/mL (113.04 mM; Need ultrasonic) |
| 过滤标签 | 表观遗传学,Polo-like Kinase (PLK),Aurora Kinase,Cell Cycle/DNA Damage |
| 储存温度 | 避光,-80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | AAPK-25 是一种强效的选择性 Aurora/PLK 双抑制剂，具有抗肿瘤活性，可导致有丝分裂延迟，使细胞停滞在原叶期，生物标志物组蛋白 H3 Ser10 磷酸化反映了这一点，随后细胞凋亡激增。抗肿瘤活性 |
| 英文描述 |
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 H3 Ser10 phosphorylation and followed by a surge in apoptosis . AAPK-25 targets Aurora-A, -B, and -C with K d values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with K d values ranging from 55-456 nM In Vitro AAPK-25 inhibits HCT-116, Calu6, A549 and MCF-7 cells growth with IC 50 s 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 H3 Ser10 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo AAPK-25 enhances survival rate in the BALB/c nude mice tumor xenograft model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target: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) |