TL 13-12 |
Catalog No.GC50560 |
TL 13-12 es un potente y selectivo degradador de ALK-PROTAC e inhibe la actividad de ALK con un valor IC50 de 0,69 nM. TL 13-12 también provoca la degradación de quinasas adicionales, incluidas Aurora A, FER, PTK2 y RPS6KA1 con valores IC50 de 13,5 nM, 5,74 nM, 18,4 nM y 65 nM, respectivamente. TL 13-12 se compone de la conjugación de TAE684 y el ligando Cereblon de Pomalidomida.
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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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