|TL13-12|CsnPharm

CAS No.: 2229037-04-9

TL13-12 Catalog No. CSN22281

TL13-12 is PROTAC selectively targeting on ALK with DC50 values of 10nM and 180nM in H3122 and Karpas 299 cells, respectively, consist of an ALK-binding TAE684 ligand linked to Pomalidomide.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述TL13-12 is PROTAC selectively targeting on ALK with DC50 values of 10nM and 180nM in H3122 and Karpas 299 cells, respectively, consist of an ALK-binding TAE684 ligand linked to Pomalidomide. TL13-12 exhibited anti-proliferative effect on H3122, Karpas 299, SU-DHL-1, Kelly, Lan5 with 21.3, 2.6, 1.4, 95 and 17nM, 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 TL13-12 on Kelly, Lan5, SH-SY5Y and CHLA20 cells. TL13-12 achieved max degradation of ALK in H3122 and Karpas 299 cells at concentration of 500nM post 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 TL13-12 (250nM) in H3122 and Karpas 299 cells. Different from TL13-112, TL13-12 exhibited degradation activity on Aurora A at concentration ranging in 20-160nM in Kelly and CHLA20 (co-treated with Tariquidar) cells post 16h. TL13-22 is a negative control for TL13-12^[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
- 1.0401 mL
- 5.2003 mL
- 10.4006 mL
- 5 mM
- 0.2080 mL
- 1.0401 mL
- 2.0801 mL
- 10 mM
- 0.1040 mL
- 0.5200 mL
- 1.0401 mL

技术信息

CAS号	2229037-04-9	储存条件	粉末液体 -20°C:3-6 月 -80°C:12月
分子式	C45H53ClN10O10S	运输	蓝冰
分子量	961.48	别名

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

TL13-12 Catalog No. CSN22281

靶点选择性

请登录您的专属账户

确认信息