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TL13-12 {[allProObj[0].p_purity_real_show]}

货号:A262353

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 化学结构 CAS号:2229037-04-9
TL13-12 化学结构
CAS号:2229037-04-9
TL13-12 3D分子结构
CAS号:2229037-04-9
TL13-12 化学结构 CAS号:2229037-04-9
TL13-12 3D分子结构 CAS号:2229037-04-9
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TL13-12 纯度/质量文件 产品仅供科研

货号:A262353 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 ALK 其他靶点 纯度
ASP3026 +

ALK, IC50: 3.5 nM

99%+
ALK-IN-1 ++++

ALK, IC50: 0.07 nM

98+%
Crizotinib ++++

ROS1, Ki: <0.025 nM

ALK, IC50: 24 nM

98%
Entrectinib 99%+
Brigatinib +++

ROS1, IC50: 1.9 nM

ALK, IC50: 0.37 nM

FLT3 98%
NVP-TAE 684 +

ALK, IC50: 3 nM

99%+
Alectinib ++

ALK (F1174L), IC50: 3.5 nM

ALK, IC50: 1.9 nM

98%
Ceritinib +++

ALK, IC50: 0.2 nM

Insulin Receptor,IGF-1R 98%
GSK1838705A +++

ALK, IC50: 0.5 nM

Insulin Receptor,IGF-1R 99%
AZD-3463 ++

ALK, Ki: 0.75 nM

IGF-1R 99%
Lorlatinib ++++

ROS1, Ki: <0.07 nM

ALK (L1196M), Ki: 0.07 nM

98%
Repotrectinib +

ALK(G1202R), IC50: 1.26 nM

ALK(L1196M), IC50: 1.01 nM

Src 99%
Belizatinib ++

ALK, IC50: 0.7 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

TL13-12 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].

TL13-12 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.

TL13-12 实验方案

计算器
存储液制备 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

TL13-12 技术信息

CAS号2229037-04-9
分子式C45H53ClN10O10S
分子量 961.481
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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