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AAPK-25

Catalog No. T10215 CAS 2247919-28-2

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.

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AAPK-25, CAS 2247919-28-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 97.00
5 mg	In stock	$ 261.00
10 mg	In stock	$ 387.00
25 mg	In stock	$ 649.00
50 mg	In stock	$ 923.00
100 mg	In stock	$ 1,260.00
500 mg	In stock	$ 2,520.00
1 mL * 10 mM (in DMSO)	In stock	$ 297.00

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Purity: 97.79%

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Description	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.
Targets&IC50	PI3K:7.11 μM (kd), PLK2:272 nM (kd), Aurora B:78 nM (kd), PLK3:456 nM (kd), Aurora A:23 nM (kd), ERK:5.32 μM (kd), Aurora C:289 nM (kd), CDK:8.02 μM , PLK1:55 nM (kd)
In vitro	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.
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (113.04 mM)

References and Literature

1. Qi B, et al. Discovery of inhibitors of Aurora/PLK targets as anti-cancer agents. J Med Chem. 2019 Aug 5.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Active Compound Library Inhibitor Library Epigenetics Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library Bioactive Compound Library Kinase Inhibitor Library

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Keywords

AAPK-25 2247919-28-2 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic PLK Aurora Kinase AAPK 25 inhibit Polo-like Kinase (PLK) AAPK25 Inhibitor inhibitor

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