TL 13-12 |
Catalog No.GC50560 |
Le TL 13-12 est un dégradeur ALK-PROTAC puissant et sélectif et inhibe l'activité ALK avec une valeur IC50 de 0,69 nM. TL 13-12 provoque également la dégradation de kinases supplémentaires, notamment Aurora A, FER, PTK2 et RPS6KA1 avec des valeurs IC50 de 13,5 nM, 5,74 nM, 18,4 nM et 65 nM, respectivement. TL 13-12 est composé de la conjugaison de TAE684 et du ligand Cereblon de Pomalidomide.
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Cas No.: 2229037-04-9
Sample solution is provided at 25 µL, 10mM.
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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