Art. -Nr.: HY-178472

AurAP14

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AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC₅₀s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC. (Pink: Aurora A ligand (HY-10971), Blue: E3 ligase Ligand (HY-W437598), Black: Linker).
(Pink: Aurora A ligand (HY-10971); Blue: Cereblon ligand (HY-W437598); Black: linker).

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Reinheit: 99.42%
CAS. Nr.: 3106831-75-5
Formel: C₅₄H₅₄Cl₂FN₁₁O₆
Molecular Weight:1042.98

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AurAP14 Chemical Structure

CAS. Nr.: 3106831-75-5

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

Biologische Aktivität

Beschreibung

AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC₅₀s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC. (Pink: Aurora A ligand (HY-10971), Blue: E3 ligase Ligand (HY-W437598), Black: Linker)^[1]. (Pink: Aurora A ligand (HY-10971); Blue: Cereblon ligand (HY-W437598); Black: linker).

IC₅₀ & Target^[1]

Aurora A

120 nM (DC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen :

In Vitro

AurAP14 (0.1-4 μM) degrades Aurora A, inhibits Aurora A-mediated phosphorylation of p53 (Ser315), and disrupts the non-catalytic protection of the proto-oncoprotein C-MYC in MCF-7and A549 cells^[1].
AurAP14 (0.5 μM, 24 h) inhibits A549 cells migration and colony formation and arrests A549 cells in the S and G2/M phases^[1].
AurAP14 (0.5 μM, 24-48 h) induces apoptosis in A549 cells^[1].

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

Cell Cycle Analysis^[1]

Cell Line:

A549 cells
Concentration:

0.5 μM
Incubation Time:

24 h
Result:

Arrested A549 cells in the S and G2/M phases.

Apoptosis Analysis^[1]

Cell Line:

A549 cells
Concentration:

0.5 μM
Incubation Time:

12, 24, 48 h
Result:

Induced apoptosis in A549 cells.

In Vivo

AurAP14 (30 mg/kg, i.p., once every 2 days, 21 days) achieves tumor growth inhibition in A549 and A549/PTR nude mouse xenograft models^[1].

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

Animal Model:

A549 cells and A549/PTR cells (1.5×10⁷ cells/100 μL) were subcutaneously implanted into the armpits of 5-week-old male BALB/c nude mice^[1]
Dosage:

30 mg/kg
Administration:

i.p., once every 2 days, 21 days
Result:

Achieved tumor growth inhibition (TGI) rates of 59.6% and 56.6% in A549 and A549/PTR nude mouse xenograft models, respectively.
Showed no significant changes in body weight and no obvious organ toxicity.
Reduced Aurora A expression in tumor tissues by more than 50%.

Chemical Information

CAS. Nr. 3106831-75-5
Appearance Solid
Molecular Weight 1042.98
Formel C₅₄H₅₄Cl₂FN₁₁O₆
Color Light yellow to yellow
SMILES

COC1=CC(NC2=NC3=C(CN=C(C4=C3C=CC(Cl)=C4)C5=C(C=CC=C5F)OC)C=N2)=CC=C1C(NCCOCCNC(CCCCCC#CC6=CN(C7=C6C(Cl)=NC(N)=N7)CC8=NC=C(C(OC)=C8C)C)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (95.88 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

0.9588 mL

4.7940 mL

9.5879 mL

5 mM

0.1918 mL

0.9588 mL

1.9176 mL

10 mM

0.0959 mL

0.4794 mL

0.9588 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. 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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (2.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (2.40 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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]. Deng XY, et al. Aurora A degradation by HSP90 interactome-mediating PROTACs in A549 and paclitaxel-resistant A549 cells. Eur J Med Chem. 2025 Dec 15;300:118141. [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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. 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	0.9588 mL	4.7940 mL	9.5879 mL	23.9698 mL
	5 mM	0.1918 mL	0.9588 mL	1.9176 mL	4.7940 mL
	10 mM	0.0959 mL	0.4794 mL	0.9588 mL	2.3970 mL
	15 mM	0.0639 mL	0.3196 mL	0.6392 mL	1.5980 mL
	20 mM	0.0479 mL	0.2397 mL	0.4794 mL	1.1985 mL
	25 mM	0.0384 mL	0.1918 mL	0.3835 mL	0.9588 mL
	30 mM	0.0320 mL	0.1598 mL	0.3196 mL	0.7990 mL
	40 mM	0.0240 mL	0.1198 mL	0.2397 mL	0.5992 mL
	50 mM	0.0192 mL	0.0959 mL	0.1918 mL	0.4794 mL
	60 mM	0.0160 mL	0.0799 mL	0.1598 mL	0.3995 mL
	80 mM	0.0120 mL	0.0599 mL	0.1198 mL	0.2996 mL

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AurAP14

PROTAC Library

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Aurora Kinase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AurAP14 Related Classifications

HY-178472 Related Classifications