AP-1

• Target:

  Others

• Related Pathways:

  Others

• Bioactivity:

  AP-1, a miniaturized proteolysis-targeting chimera (PROTAC) incorporating an anaplastic lymphoma kinase (ALK) ligand connected to (±) -thalidomide via an ultrashort linker, effectively degrades ALK fusion proteins such as NPM-ALK in Karpas-299 cells and EML4-ALK and ALKF1174L in SN-N-SH and NCI H3122 cells, respectively. Concentrations ranging from 10 to 300 nM are sufficient for its action, which is hindered by the proteasome inhibitor MG-132. Demonstrating selectivity, AP-1 exhibits cytotoxicity towards ALK-dependent Karpas-299 cells with an IC50 value of 0.1265 nM, while showing significantly less toxicity to non-ALK-dependent THP-1 cells (IC50 = 2,704 nM) . Furthermore, it effectively reduces tumor volume in NCI H3122 mouse xenograft models at doses of 25, 50, and 100 mg/kg.

• Smiles:

  O=C(CNC1=C(C(N(C2C(NC(CC2)=O)=O)C3=O)=O)C3=CC=C1)N4CCN(C5=CC(OC)=C(NC6=NC(NC7=CC=CC=C7S(C(C)C)(=O)=O)=C(Cl)C=N6)C=C5)CC4

• Molecular Formula:

  C39H40ClN9O8S

• Molecular Weight:

  830.31

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C