TL 13-12 是一种有效的选择性 ALK-PROTAC 降解剂，可抑制 ALK 活性，IC50 值为 0.69 nM。 TL 13-12 还促进其他激酶的降解，包括 Aurora A、FER、PTK2 和 RPS6KA1，IC50 值分别为 13.5 nM、5.74 nM、18.4 nM 和 65 nM。 TL 13-12 由 TAE684 和 Pomalidomide 的 Cereblon 配体的缀合组成。
Selective anaplastic lymphoma kinase (ALK) degrader (DC50 values are 10 and 180 nM in H3122 and Karpas 299 cells, respectively). Comprises the cereblon E3 ligase ligand Pomalidomide , conjugated to an ALK inhibitor. Inhibits proliferation of ALK-positive cancer cell lines. Exhibits higher selectivity for ALK over Aurora A kinase compared with TL 13 -112 (Cat.No. 6745). Maximum degradation is exhibited at 16 h. Negative control TL 13-22 also available.
Powell et al (2018) Chemically induced degradation of anaplastic lymphoma kinase (ALK). J.Med.Chem. 61 4249 PMID:29660984
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