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AAPK-25

Catalog No.GC35216

AAPK-25 est un double inhibiteur Aurora/PLK puissant et sélectif avec une activité anti-tumorale, qui peut provoquer un retard mitotique et arrêter les cellules dans une prométaphase, reflétée par la phosphorylation de l'histone H3Ser10 du biomarqueur et suivie d'une augmentation de l'apoptose. AAPK-25 cible Aurora-A, -B et -C avec des valeurs de Kd allant de 23 À 289 nM, ainsi que PLK-1, -2 et -3 avec des valeurs de Kd allant de 55 À 456 nM.

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AAPK-25 Chemical Structure

Cas No.: 2247919-28-2

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & SDS

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Background

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 H3Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with Kd values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with Kd values ranging from 55-456 nM[1]. 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)[1]

AAPK-25 inhibits HCT-116, Calu6, A549 and MCF-7 cells growth with IC50s of 0.4, 5.3, 11.6, and 2.3 μM, respectively[1].AAPK-25 induces apoptosis as a dose-dependent manner in HCT-116 cell line[1].AAPK-25 has significantly increased histone H3Ser10 phosphorylation, indicating a markedly mitotic block[1].AAPK-25 is in notably inhibition of the mitotic spindle checkpoint, which is mainly mediated by cell cycle signaling and mitotic pathways[1].

AAPK-25 enhances survival rate in the BALB/c nude mice tumor xenograft model[1].

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

Chemical Properties

Cas No. 2247919-28-2 SDF
Canonical SMILES ClC1=CC(C(NC2=CC=C(C=C(C(NC3=NC=CS3)=O)C=C4)C4=C2)=O)=CC=C1Cl
Formula C21H13Cl2N3O2S M.Wt 442.32
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.2608 mL 11.304 mL 22.6081 mL
5 mM 0.4522 mL 2.2608 mL 4.5216 mL
10 mM 0.2261 mL 1.1304 mL 2.2608 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 25 reference(s) in Google Scholar.)

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