Art. -Nr.: HY-126249

AAPK-25

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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 H3^Ser10 phosphorylation and followed by a surge in apoptosis. AAPK-25 targets Aurora-A, -B, and -C with K_d values ranging from 23-289 nM, as well as PLK-1, -2, and -3 with K_d values ranging from 55-456 nM.

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Reinheit: 98.09%
CAS. Nr.: 2247919-28-2
Formel: C₂₁H₁₃Cl₂N₃O₂S
Molecular Weight:442.32

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

AAPK-25 Chemical Structure

CAS. Nr.: 2247919-28-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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]

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen :

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	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	[PMID: 31381325]
Calu-6	IC₅₀	5.3 μM Compound: AAPK-25	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	[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	[PMID: 31381325]
MCF7	IC₅₀	2.3 μM Compound: AAPK-25	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	[PMID: 31381325]

In Vitro

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 H3^Ser10 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.

In Vivo

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 2247919-28-2
Appearance Solid
Molecular Weight 442.32
Formel C₂₁H₁₃Cl₂N₃O₂S
Color Off-white to light yellow
SMILES

ClC1=CC(C(NC2=CC=C(C=C(C(NC3=NC=CS3)=O)C=C4)C4=C2)=O)=CC=C1Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2608 mL

11.3040 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

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

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

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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AAPK-25

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AAPK-25

Anti-Blood Cancer Compound Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Alle Polo-like Kinase (PLK) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AAPK-25 Related Classifications

HY-126249 Related Classifications