AAPK-25
作者：齊岳
發(fā)布時間：2023-09-13
09:13:12
點擊數(shù)：
產(chǎn)品名稱：AAPK-25
產(chǎn)品描述：
| 產(chǎn)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. |
| 靶點活性 | 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) |
| 體外活性 | 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. |
| 體內(nèi)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 |
存儲
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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公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業(yè)務范圍包括化學試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學品、中間體和化工材料等領域。
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