TL 13-12|2229037-04-9|安捷凯

TL 13-12

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。

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

Background

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