Mice therapeutically given BP-1-102, an orally bioavailable compound targeting STAT3/NF-kB activation and cross-talk, exhibit reduced colon tumorigenesis and diminished expression of STAT3/NF-kB-activating cytokines in the neoplastic areas[2]. BP-1-102 is orally bioavailable and that the agent accumulates in tumor tissues at levels sufficient to inhibit aberrantly active Stat3 functions and inhibit tumor growth[1].
In Vitro
BP-1-102 binds Stat3 with an affinity KD of 504 nM. BP-1-102 inhibits Stat3 DNA-binding activity in vitro, with an IC50 value of 6.8±0.8 μM. It blocks Stat3-phospho-tyrosine peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8[1].
Kinase Assay
Cell Assay
Animal Administration
References
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