2229037-19-6|TL13-112|CsnPharm

CAS No.: 2229037-19-6

TL13-112 Catalog No. CSN22280

TL13-112 is PROTAC selectively targeting on ALK with DC50 values of 10nM and 40nM in H3122 and Karpas 299 cells, respectively, consist of an ALK-binding LDK378 ligand linked to Pomalidomide.

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400-920-2911

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技术信息

生物活性

描述TL13-112 is PROTAC selectively targeting on ALK with DC50 values of 10nM and 40nM in H3122 and Karpas 299 cells, respectively, consist of an ALK-binding LDK378 ligand linked to Pomalidomide. TL13-112 exhibited anti-proliferative effect on H3122, Karpas 299, SU-DHL-1, Kelly and Lan5 with 26.4, 9.2, 2.4, 374 and 934nM, respectively, post 72-hour treatment, but with much less potency to SH-SY5Y and CHLA20 cells. The co-treatment with P-gp inhibitor Tariquidar (125nM) could improve the anti-proliferative potency of TL13-112 on Kelly, Lan5, SH-SY5Y and CHLA20 cells. Degrader behavior of TL13-112 may differ from various cell lines. TL13-112 at concentration of 500nM achieved max degradation of ALK in H3122 and Karpas 299 cells at 16h, but with a significant degradation of Aurora A observed. The phosphorylation levels of ALK^Y1604 site and its downstream STAT3^Y705 phosphorylation site were decreased post 6-48h accompanied with the degradation of ALK protein by TL13-112 (250nM) in H3122 and Karpas 299 cells. However, it degraded ALK in Kelly and CHLA20 (co-treated with Tariquidar) cells without significant effect on Aurora A (at concentration<160nM), without significant change of its downstream p-STAT3^Y705 level up to 48h (at concentration of 250nM). TL13-110 is a negative control of TL13-112^[1].
参考文献

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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.9974 mL
- 4.9872 mL
- 9.9744 mL
- 5 mM
- 0.1995 mL
- 0.9974 mL
- 1.9949 mL
- 10 mM
- 0.0997 mL
- 0.4987 mL
- 0.9974 mL

技术信息

CAS号	2229037-19-6	储存条件	粉末液体 -20°C:3-6 月 -80°C:12月
分子式	C49H60ClN9O10S	运输	蓝冰
分子量	1002.57	别名

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TL13-112 Catalog No. CSN22280

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