产品说明书

TL13-112

Print
Chemical Structure| 2229037-19-6 同义名 : -
CAS号 : 2229037-19-6
货号 : A671611
分子式 : C49H60ClN9O10S
纯度 : 98%
分子量 : 1002.573
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(104.73 mM)，配合低频超声，并水浴加热至45℃助溶，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 TL13-112 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 ALKY1604 site and its downstream STAT3Y705 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-STAT3Y705 level up to 48h (at concentration of 250nM). TL13-110 is a negative control of TL13-112[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.00mL

0.20mL

0.10mL

4.99mL

1.00mL

0.50mL

9.97mL

1.99mL

1.00mL
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.