TL13-112,2229037-19-6

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TL13-112

CAS No. : 2229037-19-6

MCE 国际站：TL13-112

产品活性：TL13-112 是一种有效的选择性 ALK-PROTAC 降解物，可抑制 ALK 活性，IC₅₀ 值 0.14 nM，并促进包括 Aurora A、FER、PTK2 和 RPS6KA1 在内的其他激酶的降解，IC₅₀ 值分别 8550 nM、42.4 nM、25.4 nM 和 677 nM。TL13-112 由 Ceritinib (HY-15656) 和 Cereblon 配体 Pomalidomide (HY-10984) 结合而成。

研究领域：PROTAC  |  Protein Tyrosine Kinase/RTK

作用靶点：PROTACs  |  Anaplastic lymphoma kinase (ALK)

In Vitro: 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.

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