TL 13-12 |
رقم الكتالوجGC50560 |
TL 13-12 عبارة عن مطهر ALK-PROTAC قوي وانتقائي ويثبط نشاط ALK بقيمة IC50 تبلغ 0.69 نانومتر. يدفع TL 13-12 أيضًا إلى تدهور كينازات إضافية بما في ذلك Aurora A و FER و PTK2 و RPS6KA1 بقيم IC50 البالغة 13.5 نانومتر و 5.74 نانومتر و 18.4 نانومتر و 65 نانومتر ، على التوالي. يتكون TL 13-12 من اقتران TAE684 ورابط Cereblon لـ 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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