AAPK-25
Based on 1 Customer Validation
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.
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- Pureza: 98.09%
- No. CAS: 2247919-28-2
- Fòrmula: C21H13Cl2N3O2S
- Peso molecular:442.32
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Ver todos los productos específicos de isoformas Aurora Kinase
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Actividad biológica
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]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
11.6 μM
Compound: AAPK-25
|
Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay
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[PMID: 31381325] |
| Calu-6 | IC50 |
5.3 μM
Compound: AAPK-25
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Antiproliferative activity against human Calu6 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human Calu6 cells measured after 48 hrs by MTT assay
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[PMID: 31381325] |
| HCT-116 | IC50 |
0.4 μM
Compound: AAPK-25
|
Antiproliferative activity against human HCT116 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells measured after 48 hrs by MTT assay
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[PMID: 31381325] |
| MCF7 | IC50 |
2.3 μM
Compound: AAPK-25
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Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay
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[PMID: 31381325] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2247919-28-2
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Appearance Solid
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Peso molecular 442.32
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Fòrmula C21H13Cl2N3O2S
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Color Off-white to light yellow
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SMILES
ClC1=CC(C(NC2=CC=C(C=C(C(NC3=NC=CS3)=O)C=C4)C4=C2)=O)=CC=C1Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 50 mg/mL (113.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2608 mL | 11.3040 mL | 22.6081 mL | 56.5202 mL |
| 5 mM | 0.4522 mL | 2.2608 mL | 4.5216 mL | 11.3040 mL | |
| 10 mM | 0.2261 mL | 1.1304 mL | 2.2608 mL | 5.6520 mL | |
| 15 mM | 0.1507 mL | 0.7536 mL | 1.5072 mL | 3.7680 mL | |
| 20 mM | 0.1130 mL | 0.5652 mL | 1.1304 mL | 2.8260 mL | |
| 25 mM | 0.0904 mL | 0.4522 mL | 0.9043 mL | 2.2608 mL | |
| 30 mM | 0.0754 mL | 0.3768 mL | 0.7536 mL | 1.8840 mL | |
| 40 mM | 0.0565 mL | 0.2826 mL | 0.5652 mL | 1.4130 mL | |
| 50 mM | 0.0452 mL | 0.2261 mL | 0.4522 mL | 1.1304 mL | |
| 60 mM | 0.0377 mL | 0.1884 mL | 0.3768 mL | 0.9420 mL | |
| 80 mM | 0.0283 mL | 0.1413 mL | 0.2826 mL | 0.7065 mL | |
| 100 mM | 0.0226 mL | 0.1130 mL | 0.2261 mL | 0.5652 mL |
AAPK-25 Related Classifications
HY-126249 Related Classifications
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