SH5-07

一种STAT3抑制剂（Ki=10.46µM），对STAT3的选择性高于STAT1（STAT1的Ki>100µM）；能够抑制NIH3T3成纤维细胞核提取物中持续活化的STAT3与DNA的结合（IC50=3.9µM）；对AR230细胞和伊马替尼耐药的AR230细胞具有细胞毒性（IC50分别为8.1µM和7µM），并对多种胶质母细胞瘤干细胞（CSCs）表现出细胞毒性（IC50为0.195-1.12µM）；在3mg/kg和5mg/kg的剂量下，分别减少MDA-MB-231乳腺癌和U-251MG胶质母细胞瘤小鼠异种移植模型中的肿瘤生长；在5µM浓度下对弓形虫（T.gondii）具有活性。A STAT3 inhibitor (Ki = 10.46 µM); selective for STAT3 over STAT1 (Ki = >100 µM); prevents constitutively active STAT3 DNA binding in NIH3T3 fibroblast nuclear extracts (IC50 = 3.9 µM); cytotoxic to AR230 and imatinib-resistant AR230 cells (IC50s = 8.1 and 7 µM, respectively) and a variety of glioblastoma CSCs (IC50s = 0.195-1.12 µM); reduces tumor growth in MDA-MB-231 breast cancer and U-251MG glioblastoma mouse xenograft models at 3 and 5 mg/kg, respectively; active against T. gondii at 5 µM.分子式C29H28F5N3O5S分子量625.6O=C(C1=CC=C(N(CC2=CC=C(C3CCCCC3)C=C2)C(CN(S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=O)C)=O)C=C1)NO