AAPK-25 |
| رقم الكتالوجGC35216 |
AAPK-25 هو مثبط مزدوج قوي وانتقائي Aurora / PLK مع نشاط مضاد للورم ، والذي يمكن أن يتسبب في تأخير الانقسام وتوقف الخلايا في مرحلة ما قبل الطور ، مما يعكسه الفسفرة هيستون H3Ser10 للعلامة الحيوية ويتبعها زيادة في موت الخلايا المبرمجتستهدف AAPK-25 Aurora-A و -B و -C بقيم Kd تتراوح من 23-289 نانومتر ، بالإضافة إلى PLK-1 و -2 و -3 بقيم Kd تتراوح من 55-456 نانومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2247919-28-2
Sample solution is provided at 25 µL, 10mM.
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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.
| 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 |
| الذوبان | 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. | ||
| Prepare stock solution | |||
|
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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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