TL 13-12

TL13-12 is a novel Anaplastic Lymphoma Kinase (ALK)-PROTAC developed through conjugation of TAE684 and the cereblon ligand pomalidomide; also promotes the degradation of additional kinases including PTK2 (FAK), Aurora A, FER, and RPS6KA1 (RSK1).

Research Areas >> Cancer

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> ALK

IC50: 0.69 nM (ALK)[1]

TL13-12 (0-200 nM; 16 hours)  is selective for degradation of ALK with the DC50s of 10 nM and 180 nM in H3122 cell and Karpas 299, respectively[1]. TL13-12 (0-160 nM; 16 hours) degrades ALK and aurora A protein expression as a dose-dependent manner in Kelly and CHLA20 cells[1]. TL13-12 (100 nM; 16 hours) significantly inhibits Tariqudan-induced ALK and Aurora A protein expression in CHLA20 cells[1]. Western Blot Analysis[1] Cell Line: Kelly and CHLA20 cells Concentration: 0 nM; 20 nM; 40 nM; 60 nM; 80 nM; 100 nM; 140 nM; 160 nM Incubation Time: 16 hours Result: Exhibited degrader behavior in cells. Western Blot Analysis[1] Cell Line: CHLA20 cells Concentration: 100 nM Incubation Time: 16 hours Result: Decreased ALK and Aurora A protein expression.

[1]. Powell CE, et al. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).J Med Chem. 2018 May 10;61(9):4249-4255.