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AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, causing mitotic delay and arresting cells in prometaphase, followed by increased apoptosis. It targets Aurora-A/-B/-C with Kd values ranging from 23-289 nM.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $87 | In Stock | |
5 mg | $212 | In Stock | |
10 mg | $318 | In Stock | |
25 mg | $579 | In Stock | |
50 mg | $868 | In Stock | |
100 mg | $1,260 | In Stock | |
1 mL x 10 mM (in DMSO) | $245 | In Stock |
Description | AAPK-25 is a potent and selective Aurora/PLK dual inhibitor with anti-tumor activity, causing mitotic delay and arresting cells in prometaphase, followed by increased apoptosis. It targets Aurora-A/-B/-C with Kd values ranging from 23-289 nM. |
Targets&IC50 | Aurora C:289 nM (kd), Aurora A:23 nM (kd), ERK:5.32 μM (kd), Aurora B:78 nM (kd), PLK3:456 nM (kd), PI3K:7.11 μM (kd), PLK2:272 nM (kd), CDK:8.02 μM , PLK1:55 nM (kd) |
In vitro | AAPK-25 inhibits the growth of HCT-116, Calu6, A549, and MCF-7 cells (IC50s: 0.4, 5.3, 11.6, and 2.3 μM). It induces apoptosis in a dose-dependent manner in the HCT-116 cell line, significantly increases histone H3Ser10 phosphorylation, indicating a marked mitotic block, and notably inhibits the mitotic spindle checkpoint. |
In vivo | AAPK-25 enhances the survival rate in the BALB/c nude mice tumor xenograft model. |
Molecular Weight | 442.32 |
Formula | C21H13Cl2N3O2S |
Cas No. | 2247919-28-2 |
Smiles | Clc1ccc(cc1Cl)C(=O)Nc1ccc2cc(ccc2c1)C(=O)Nc1nccs1 |
Relative Density. | 1.536 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (113.04 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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