TL 13-112 是一种有效的选择性 ALK-PROTAC 降解剂，抑制 ALK 活性，IC50 值为 0.14 nM。 TL 13-112 还促进其他激酶的降解，包括 Aurora A、FER、PTK2 和 RPS6KA1，IC50 值分别为 8550 nM、42.4 nM、25.4 nM 和 677 nM。 TL 13-112 由色瑞替尼和 Pomalidomide 的 Cereblon 配体的结合物组成。
Selective anaplastic lymphoma kinase (ALK) degrader (DC50 values are 10 and 40 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. Maximum degradation exhibited at 16 h. Negative control TL 13-110 also available.
Powell et al (2019) Chemically induced degradation of anaplastic lymphoma kinase (ALK). J.Med.Chem. 61 4249 PMID:29660984
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