2. PROTAC Cell Cycle/DNA Damage Epigenetics
  3. PROTACs Aurora Kinase
  4. AurAP14

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).

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

AurAP14

AurAP14 Chemical Structure

CAS No. : 3106831-75-5

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Based on 1 publication(s) in Google Scholar

AurAP14 Related Antibodies

Top Publications Citing Use of Products

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Aurora Kinase Aurora A Aurora B Aurora C

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target[1]

Aurora A

120 nM (DC50)

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.

AurAP14 Related Antibodies

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%.
Molecular Weight

1042.98

Formula

C54H54Cl2FN11O6
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9588 mL 4.7940 mL 9.5879 mL
5 mM 0.1918 mL 0.9588 mL 1.9176 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. 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:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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. 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 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:

AurAP143106831-75-5AurAP 14AurAP-14PROTACsAurora KinaseAurora APROTACdegraderA549A549/PTRMCF-7 cellscancerInhibitorinhibitorinhibit

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