AAPK-25
作者：齐岳
发布时间：2023-09-13
09:13:12
点击数：
产品名称：AAPK-25
产品描述：
| 产品描述 | AAPK-25, a potent and selective dual inhibitor of Aurora/PLK, causes mitotic delay and cell arrest in prometaphase, via phosphorylation of the biomarker histone H3Ser10, followed by a surge in apoptosis. AAPK-25 targets Aurora A, Aurora B, and Aurora C with Kd values ranging from 23-289 nM, and PLK1, PLK2, and PLK3 with Kd values ranging from 55-456 nM. AAPK-25 has antitumor activity. |
| 靶点活性 | PI3K:7.11 μM (kd), PLK-1:55 nM (kd), Aurora-A:23 nM (kd), PLK-2:272 nM (kd), ERK:5.32 μM (kd), Aurora-C:289 nM (kd), CDK:8.02 μM , PLK-3:456 nM (kd), Aurora-B:78 nM (kd) |
| 体外活性 | AAPK-25 inhibits HCT-116, Calu6, A549, and MCF-7 cells growth (IC50s: 0.4, 5.3, 11.6, and 2.3 μM). 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 notably inhibition of the mitotic spindle checkpoint. |
| 体内活性 | AAPK-25 enhances the survival rate in the BALB/c nude mice tumor xenograft model. |
| 分子量 | 442.32 |
| 分子式 | C21H13Cl2N3O2S |
| CAS No. | 2247919-28-2 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 50 mg/mL (113.04 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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