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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-STAT-LLY17
LLY17

Chemical Structure : LLY17

CAS No.: 1556861-34-7

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LLY17 (Compound 9)

货号: PC-24625Not For Human Use, Lab Use Only.

LLY17 (Compound 9) is an orally available, potent, and selective STAT3, directly and selectively inhibited the pY705 site of STAT3 with Ki of 400 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LLY17 (Compound 9) is an orally available, potent, and selective STAT3, directly and selectively inhibited the pY705 site of STAT3 with Ki of 400 nM.
LLY17 is highly selective in targeting of cancer cells with IC50 of 0.7 uM against MDA-MB-231, >150 fold selective over MCF-10A normal breast epithelial cells.
LLY17 inhibits multiple types of cancer cells, i.e., the UW426, UW288-1, BKPC3, MDA-MB-231, and U2OS cell lines.
LLY17 directly bound to the STAT3 protein with a Ki value of 2.42 ± 0.26 μM. The ligand:protein molar ratio was determined to be 1:1.
LLY17 selectively inhibited pY705-STAT3 protein. selectively inhibited p-STAT3(Y705) and interleukin 6 (IL-6)-induced phosphorylation of STAT3, without any inhibition of p-STAT1(Y701).
LLY17 induced the expression of STAT3 phosphatase (SHP-1), blocked STAT3 nuclear translocation.
LLY17 (2.5 mg/kg, 5 mg/kg) induced significant antitumor responses in vivo.

物理化学性质&存储条件

分子量 412.46
分子式 C20H20N4O4S
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

5,8-dioxo-6-((2-(piperazin-1-yl)phenyl)amino)-5,8-dihydronaphthalene-1-sulfonamide

参考文献

1. Wenying Yu, et al. J Med Chem. 2017 Apr 13;60(7):2718-2731.

2. Pan L, et al. Breast Cancer Res Treat. 2020 May;181(1):31-41.

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