| In Vitro | In vitro activity: C188-9 is a potent small-molecule inhibitor of STAT3 that targets the phosphotyrosyl peptide binding site within the Stat3 Src homology 2 (SH2) domain with Ki 136 nM. It does not inhibit upstream Jak or Src kinases.
Kinase Assay:
Cell Assay: UM-SCC-17B cells were incubated with various doses (0/0.1/0.3/1/3/10/30μM) of C188 or C188-9 for 24 hrs. |
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| In Vivo | Treatment of nude mice bearing xenografts of UM-SCC-17B, a radioresistant HNSCC line, with C188-9, but not C188, prevented tumor xenograft growth. C188-9 was well tolerated in mice, showed good oral bioavailability, and was concentrated in tumors. |
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| Animal model | CD2F1 female mice received isogenic C26 tumor cell via s.c injection |
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| Formulation & Dosage | D5W (5g of dextrose in 100 ml of water); 12.5 mg/kg; i.p. |
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| References | Oncotarget. 2016 May 3;7(18):26307-30; J Biol Chem. 2015 Apr 24;290(17):11177-87 |
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