2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. Aurora Kinase Polo-like Kinase (PLK) Apoptosis
  4. AAPK-25

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.

For research use only. We do not sell to patients.

AAPK-25 Chemical Structure

AAPK-25 Chemical Structure

CAS No. : 2247919-28-2

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5 mg USD 258 In-stock
10 mg USD 388 In-stock
25 mg USD 700 In-stock
50 mg USD 1050 In-stock
100 mg USD 1575 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

AAPK-25 Related Antibodies

Top Publications Citing Use of Products

View All Aurora Kinase Isoform Specific Products:

View All Isoforms
Aurora Kinase Aurora A Aurora B Aurora C

View All Polo-like Kinase (PLK) Isoform Specific Products:

View All Isoforms
PLK1 PLK2 PLK3 PLK4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

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]
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 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.

AAPK-25 Related Antibodies
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.
Molecular Weight

442.32

Formula

C21H13Cl2N3O2S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2608 mL 11.3040 mL 22.6081 mL
5 mM 0.4522 mL 2.2608 mL 4.5216 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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AAPK-25 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AAPK-252247919-28-2AAPK25AAPK 25Aurora KinasePolo-like Kinase (PLK)ApoptosisInhibitorinhibitorinhibit

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