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C188-9

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Chemical Structure| 432001-19-9 同义名 : TTI-101
CAS号 : 432001-19-9
货号 : A445130
分子式 : C27H21NO5S
纯度 : 99%+
分子量 : 471.524
MDL号 : MFCD03141581
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(53.02 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
靶点

  • STAT3

    STAT3, Kd:4.7 nM
描述 Signal transducers and activators of transcription (STATs) are a family of transcription factors essential for the pathogenesis of many cancers. STAT3 in particular has been found to be a critical mediator in the pathogenesis of many tumors. C188-9 is a STAT3 inhibitor by inhibiting STAT3 tyrosine phosphorylation. Acute myeloid leukemia (AML) cell lines treated with increasing doses of the C188-9 for 24h and EC50 values of the 7 acute myeloid leukemia cell lines varied between 6 and 8 μM in GDM-1 and Kasumi-1 cells to more than 43 μM in K562 cells. C188-9 inhibited G-CSF-induced Stat3 phosphorylation in a dose-dependent manner, with IC50 values ranging between 8 and 18 μM in primary pediatric AML cells[3]. CC188-9 reduced cell viability of all three Hepatoma cell lines with IC50 values of 11.27, 10.19 and 11.83 μM for Huh7, PLC/PRF/5 and HepG2, respectively. Intraperitoneal injection of C188-9 (100mg/kg) by daily for 4 weeks to hepatocyte-specific Pten deletion (HepPten-) mouse model inhibited tumor growth (249.02 mm3 and 106.48 mm3 for vehicle- and C188-9-treated mice, respectively; p = 0.04)[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.60mL

2.12mL

1.06mL

21.21mL

4.24mL

2.12mL
参考文献

[1]Jung KH, Yoo W, et al. Multi-functional effects of a small-molecule STAT3 inhibitor on NASH and HCC in mice. Clin Cancer Res. 2017 May 22. pii: clincanres.2253.2016.

[2]Bharadwaj U, Eckols TK, et al. Small-molecule inhibition of STAT3 in radioresistant head and neck squamous cell carcinoma. Oncotarget. 2016 May 3;7(18):26307-30.

[3]Redell MS, Ruiz MJ, Alonzo TA, Gerbing RB, Tweardy DJ. Stat3 signaling in acute myeloid leukemia: ligand-dependent and -independent activation and induction of apoptosis by a novel small-molecule Stat3 inhibitor. Blood. 2011 May 26;117(21):5701-9. doi: 10.1182/blood-2010-04-280123. Epub 2011 Mar 29. PMID: 21447830; PMCID: PMC3110027.

[4]Jung KH, Yoo W, Stevenson HL, Deshpande D, Shen H, Gagea M, Yoo SY, Wang J, Eckols TK, Bharadwaj U, Tweardy DJ, Beretta L. Multifunctional Effects of a Small-Molecule STAT3 Inhibitor on NASH and Hepatocellular Carcinoma in Mice. Clin Cancer Res. 2017 Sep 15;23(18):5537-5546. doi: 10.1158/1078-0432.CCR-16-2253. Epub 2017 May 22. PMID: 28533225; PMCID: PMC5873583.