TL13-12

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

TL13-12 

TL13-12 是一种强效的 ALK-PROTAC 降解物，抑制 ALK 活性，其 IC50 值为 0.69 nM，并促进其他激酶的降解，包括 Aurora A、FER、PTK2 和 RPS6KA1，其 IC50 值分别为 13.5 nM、5.74 nM、18.4 nM 和 65 nM。TL13-12 由 TAE684 (HY-10192) 和 Cereblon 配体 Pomalidomide (HY-10984) 结合而成。

TL13-12

TL13-12 Chemical Structure

CAS No. : 2229037-04-9

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生物活性

TL13-12 is a potent and selective ALK-PROTAC degrader and inhibits ALK activity with an IC50 value of 0.69 nM. TL13-12 also prompts the degradation of additional kinases including Aurora A, FER, PTK2, and RPS6KA1 with IC50 values of 13.5 nM, 5.74 nM, 18.4 nM, and 65 nM, respectively. TL13-12 is comprised of the conjugation of TAE684 (HY-10192) and the Cereblon ligand of Pomalidomide (HY-10984)[1].

IC50 & Target

Cereblon

1.2 μM (IC50)

体外研究
(In Vitro)

TL13-12 (0-200 nM; 16 hours)  is selective for degradation of ALK with the DC50s of 10 nM and 180 nM in H3122 cell and Karpas 299, respectively[1].
TL13-12 (0-160 nM; 16 hours) degrades ALK and aurora A protein expression as a dose-dependent manner in Kelly and CHLA20 cells[1].
TL13-12 (100 nM; 16 hours) significantly inhibits Tariqudan-induced ALK and Aurora A protein expression in CHLA20 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Kelly and CHLA20 cells
Concentration: 0 nM; 20 nM; 40 nM; 60 nM; 80 nM; 100 nM; 140 nM; 160 nM
Incubation Time: 16 hours
Result: Exhibited degrader behavior in cells.

Western Blot Analysis[1]

Cell Line: CHLA20 cells
Concentration: 100 nM
Incubation Time: 16 hours
Result: Decreased ALK and Aurora A protein expression.

分子量

961.48

Formula

C45H53ClN10O10S
CAS 号

2229037-04-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Powell CE, et al. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).J Med Chem. 2018 May 10;61(9):4249-4255.

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