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

AAPK-25 

Cat. No.: HY-126249 Purity: 98.31%
COA Handling Instructions

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

Size Price Stock Quantity
1 mg USD 180 In-stock
5 mg USD 380 In-stock
10 mg USD 620 In-stock
25 mg USD 1250 In-stock
50 mg USD 2000 In-stock
100 mg USD 3200 In-stock
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This product is a controlled substance and not for sale in your territory.

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Based on 1 publication(s) in Google Scholar

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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]

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.

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

Appearance

Solid

Formula

C21H13Cl2N3O2S

CAS No.
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)

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
10 mM 0.2261 mL 1.1304 mL 2.2608 mL
*Please refer to the solubility information to select the appropriate solvent.
Purity & Documentation
References
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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.

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Product Name:
AAPK-25
Cat. No.:
HY-126249
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