TL13-12

TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC₅₀ value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC₅₀ values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the Cereblon ligand of Pomalidomide (HY-10984)^[1]. IC50 & Target:IC50: 0.69 nM (ALK)^[1] In Vitro: 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].