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) [1].
Product Specifications
UNSPSC
12352005
Target
Aurora Kinase; PROTACs
Related Pathways
Cell Cycle/DNA Damage; Epigenetics; PROTAC
Applications
Cancer-Kinase/protease
Field of Research
Cancer
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
Molecular Formula
C54H54Cl2FN11O6
Molecular Weight
1042.98
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Aurora A
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