Chemical Structure : ODZ10117
货号: PC-47064Not For Human Use, Lab Use Only.
ODZ10117 is a small molecule inhibitor of STAT3, effectively inhibits the level of tyrosine phosphorylated STAT3 in various cancer cell lines.
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ODZ10117 is a small molecule inhibitor of STAT3, effectively inhibits the level of tyrosine phosphorylated STAT3 in various cancer cell lines.
ODZ10117 binds to the phospho-tyrosine binding pocket on the SH2 domain of STAT3 with a docking score of -6.17 kcal/mol and participated in many interactions with surrounding residues of the SH2 domain.
ODZ10117 significantly decreased the homodimerization of STAT3, inhibited the transcriptional activity of STAT3 in a concentration-dependent manner with IC50 of 7.5 uM in in MDA-MB-231 cells.
ODZ10117 did not significantly inhibit the JAK family of tyrosine kinases, including JAK1, JAK2, JAK3, and TYK2, in breast cancer cells and Hodgkin's lymphoma cells.
ODZ10117 induces apoptotic cell death and decreases migration and invasion of breast cancer.
ODZ10117 (1-10 mg/kg, 5 times a week for 23 days) suppressed tumor growth in breast cancer xenograft models, inhibits tumor growth and lung metastasis and increases survival in breast cancer xenograft model.
分子量 | 362.412 | |
分子式 | C10H5Cl5N2O2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Kim BH, et al. J Clin Med. 2019 Nov 2;8(11):1847.
2. Kim BH, et al. Cells. 2020 Mar 15;9(3):722.
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