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Catalog Number | orb1980009 |
---|---|
Category | Small Molecules |
Description | 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. |
Purity | 98.00% |
MW | 830.31 |
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 |
Formula | C39H40ClN9O8S |
Biological Activity | 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. |
Storage | -20°C |
Note | For research use only |
Expiration Date | 12 months from date of receipt. |
FC, IF, IHC-Fr, IHC-P | |
Bovine, Canine, Porcine, Rabbit, Sheep | |
Human, Mouse, Rat | |
Rabbit | |
Polyclonal | |
Unconjugated |
IF, IHC-Fr, IHC-P | |
Bovine, Canine, Equine, Porcine, Rabbit | |
Human, Mouse, Rat | |
Rabbit | |
Polyclonal | |
Unconjugated |
ICC, IF, IHC-Fr, IHC-P, WB | |
Bovine, Canine, Equine, Porcine, Rabbit | |
Human, Mouse, Rat | |
Rabbit | |
Polyclonal | |
Unconjugated |
FC, IF, IHC-Fr, IHC-P, WB | |
Bovine, Canine, Gallus, Porcine, Sheep | |
Human, Mouse, Rat | |
Rabbit | |
Polyclonal | |
Unconjugated |