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TL 13-12
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TL 13-12图片
CAS NO:2229037-04-9
包装:5mg
市场价:3150元

产品介绍
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。
Cas No.2229037-04-9
Canonical SMILESCOC1=C(C=CC(N2CCN(CC2)CCOCCOCCNC(CNC3=C4C(N(C(C4=CC=C3)=O)C5CCC(NC5=O)=O)=O)=O)=C1)NC6=NC=C(C(NC7=C(S(=O)(C(C)C)=O)C=CC=C7)=N6)Cl
分子式C45H53ClN10O10S
分子量961.48
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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