A STAT3 inhibitor
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BP-1-102 is an inhibitor of STAT3.1 It binds to STAT3 (Kd = 504 nM) and inhibits STAT3 binding to an IL-6R/gp130 peptide in a fluorescence polarization assay (IC50 = 4.1 ?M). BP-1-102 (10-30 ?M) decreases viability and proliferation of STAT3-dependent NIH3T3/v-Src, MDA-MB-231, PANC-1, DU145 and A549 cancer cells, but not STAT3-independent NIH3T3, NIH3T3/vRas, TE-71, and A2780S cancer cells. It reduces tumor growth and inhibits expression of the STAT3-dependent genes encoding c-Myc, survivin, Bcl-xL, cyclin D1, and VEGF in MDA-MB-231 and A549 mouse xenograft models when administered at doses of 1 and 3 mg/kg.
1.Zhang, X., Yue, P., Page, B.D., et al.Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenograftsProc. Natl. Acad. Sci. USA109(24)9623-9628(2012)
Cell experiment: | Proliferating cells in 6- or 96-well plates are treated once with 0-30 μM BP-1-102 for 24 h or with 10 μM BP-1-102 for up to 96 h. Viable cells are counted by trypan blue exclusion/phase-contrast microscopy or assessed by a cell proliferation kit[1]. |
Animal experiment: | Mice: Athymic nude mice with established tumors are grouped and then given BP-1-102 (in 0.05% DMSO in water) at 1 or 3mg/kg (i.v.) every 2 or every 3 d or 3 mg/kg (oral gavage, 100 μL) every day for 15 or 20 d. Animals are monitored every day, and tumor sizes are measured with calipers and body weights are taken every 2 or 3 d. For each treatment group, the tumor volumes for each set of measurements are statistically analyzed in comparison with the control group using a paired T test[1]. |
参考文献: [1]. Zhang X, et al. Orally bioavailable small-molecule inhibitor of transcription factor Stat3 regresses human breast and lung cancer xenografts. Proc Natl Acad Sci U S A. 2012 Jun 12;109(24):9623-8. |
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