产品
编 号:F280125
分子式:C45H53ClN10O10S
分子量:961.48
产品类型
结构图
CAS No: 2229037-04-9
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产品详情
生物活性:
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).
体外研究:
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.TL13-12 (0-160 nM; 16 hours) degrades ALK and aurora A protein expression as a dose-dependent manner in Kelly and CHLA20 cells.TL13-12 (100 nM; 16 hours) significantly inhibits Tariqudan-induced ALK and Aurora A protein expression in CHLA20 cells.