BP-1-102

BP-1-102 is an inhibitor of STAT3. 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 µM). BP-1-102 (10-30 µM) 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.Formal Name: 4-[[(4-cyclohexylphenyl)methyl][2-[methyl[(2,3,4,5,6-pentafluorophenyl)sulfonyl]amino]acetyl]amino]-2-hydroxy-benzoic acid. CAS Number: 1334493-07-0. Molecular Formula: C29H27F5N2O6S. Formula Weight: 626.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 15 mg/ml. SMILES: OC1=CC(N(C(CN(C)S(C2=C(F)C(F)=C(F)C(F)=C2F)(=O)=O)=O)CC3=CC=C(C4CCCCC4)C=C3)=CC=C1C(O)=O. InChi Code: InChI=1S/C29H27F5N2O6S/c1-35(43(41,42)28-26(33)24(31)23(30)25(32)27(28)34)15-22(38)36(19-11-12-20(29(39)40)21(37)13-19)14-16-7-9-18(10-8-16)17-5-3-2-4-6-17/h7-13,17,37H,2-6,14-15H2,1H3,(H,39,40). InChi Key: WNVSFFVDMUSXSX-UHFFFAOYSA-N.