TL13-112

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TL13-112 是一种新型间变性淋巴瘤激酶 (ALK)-PROTAC，通过 LDK378 和 cereblon 配体泊马度胺缀合而开发。

TL13-112 is a novel Anaplastic Lymphoma Kinase (ALK)-PROTAC developed through conjugation of LDK378 and the cereblon ligand pomalidomide; also promotes the degradation of additional kinases including PTK2 (FAK), Aurora A, FER, and RPS6KA1 (RSK1).

TL13-112 binds to cereblon with an IC50 value of 2.4 uM.TL13-112 (0.01 μM-1 μM; 16 hours)?is selective for degradation of ALK with the DC50s of 10 nM and 40 nM in H3122 cell and Karpas 299, respectively. ALK degradation acts at 4 hours of treatment in H3122 cells and at 8 hours of treatment in Karpas 299 cells. The maximum degradation achieves at 16 hours in both cell lines. .TL13-112 (0.01 μM-1 μM; 16 hours) inhibits PTK2, ALK, FER, RPS6KA1 and Aurora A expression as a dose-dependent manner in H3122, Karpas 299, and Kelly cells. Western Blot Analysis Cell Line:H3122 and Karpas 299 cells Concentration:0.01 μM; 0.05 μM; 0.1 μM; 0.5 μM; 1 μM Incubation Time:16 hours Result:Inhibited ALK and Aurora A expression completely at 1 μM.Western Blot Analysis Cell Line:H3122 and Karpas 299 cells Concentration:0.01 μM; 0.05 μM; 0.1 μM; 0.5 μM; 1 μM Incubation Time:16 hours Result:Decreased PTK2, ALK, FER, RPS6KA1 and Aurora A expression.

——

——

PROTACs

PROTAC

PROTAC

——

——

2229037-19-6

1002.582

C49H60ClN9O10S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (99.74 mM)

CC1=CC(=C(C=C1C2CCN(CC2)CCOCCOCCNC(=O)CNC3=CC=CC4=C3C(=O)N(C4=O)C5CCC(=O)NC5=O)OC(C)C)NC6=NC=C(C(=N6)NC7=CC=CC=C7S(=O)(=O)C(C)C)Cl

N-(2-(2-(2-(4-(4-((5-Chloro-4-((2-(isopropylsulfonyl)phenyl)-amino)pyrimidin-2-yl)amino)-5-isopropoxy-2-methylphenyl)-piperidin-1-yl)ethoxy)ethoxy)ethyl)-2-((2-(2,6-dioxopiperidin3-yl)-1,3-dioxoisoindolin-4-yl)amino)acetamide

(-20℃)

With Ice Pack

≥ 2 years