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

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AurAP14 Related Antibodies

Top Publications Citing Use of Products

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Aurora Kinase Aurora A Aurora B Aurora C

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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
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

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AurAP14 Related Classifications

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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.

Keywords:

AurAP14AurAP 14AurAP-14PROTACsAurora KinaseAurora APROTACdegraderA549A549/PTRMCF-7 cellscancerInhibitorinhibitorinhibit

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