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TX1-85-1

Chemical Structure : TX1-85-1

CAS No.: 1603845-32-4

TX1-85-1 (Her3 (ErbB3) inhibitor)

货号: PC-38536Not For Human Use, Lab Use Only.

TX1-85-1 is a potent, selective, irreversible and covalent inhibitor of pseudokinase Her3 (ErbB3) with IC50 of 23 nM in FRET-based binding assay.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TX1-85-1 is a potent, selective, irreversible and covalent inhibitor of pseudokinase Her3 (ErbB3) with IC50 of 23 nM in FRET-based binding assay.
TX1-85-1 covalently modifies Cys721 of Her3 in vitro and in cells.
TX1-85-1 is insufficient to inactivate the Her3/PI3K/AKT pathway explaining lack of growth inhibition for Her3 dependent cells.
TX1-85-1 arrested cell proliferation, inhibited the in vitro tumorigenicity, and lead to loss of stemness in the conversion of induced pluripotent stem cells (iPSCs) into cancer stem cells (CSCs).

物理化学性质&存储条件

分子量 580.693
分子式 C32H36N8O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(5-(1-(4-(4-Acetylpiperazin-1-yl)cyclohexyl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-2-phenoxyphenyl)acrylamide

参考文献

1. Xie T, et al. Nat Chem Biol. 2014 Dec;10(12):1006-12.

2. Lim SM, et al. Bioorg Med Chem Lett. 2015 Aug 15;25(16):3382-9.

3. Hassan G, et al. Sci Rep. 2022 Feb 17;12(1):2711.

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