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TL13-12

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Chemical Structure| 2229037-04-9 同义名 : -
CAS号 : 2229037-04-9
货号 : A262353
分子式 : C45H53ClN10O10S
纯度 : 98%
分子量 : 961.481
MDL号 : N/A
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(109.21 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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 ALKY1604 site and its downstream STAT3Y705 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.04mL

0.21mL

0.10mL

5.20mL

1.04mL

0.52mL

10.40mL

2.08mL

1.04mL
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.