| Bioactivity | STAT3-IN-17 is a moderate STAT3 inhibitor (IC50=0.7 μM; HEK-Blue IL-6), with antiproliferative activity in HeLa cells. STAT3-IN-17 has good pharmacokinetic characteristics. STAT3-IN-17 also inhibits pyruvate-ferredoxin oxidoreductase (PFOR), and inhibits Helicobacter pylori[1][2]. |
| Invitro | STAT3-IN-17 (化合物 15) (10 μM; 20 h, 48 h) 抑制 STAT3 通路,抑制率为 76.5%,同时抑制 HEK-Blue IL-6 细胞活力至 15%[1]。STAT3-IN-17 (2.5-40 μM; 24 h) 抑制 STAT3 的磷酸化 (Y705)[1]。STAT3-IN-17 (10 μM, 50 μM; 48 h) 抑制 HEK 293T 细胞生长,抑制 HeLa 细胞生长,IC50 值为 2.7 μM[1]。(D)-PPA 1(化合物 24) 抑制微生物幽门螺杆菌和空肠弯曲杆菌,MIC 值分别为 1.6 μM 和 4.7 μM[2]。 |
| In Vivo | STAT3-IN-17 (化合物 15) (5 mg/kg 灌胃给药, 或 25 mg/kg 静脉注射; 单剂量) 在大鼠体内表现出优于 Nitazoxanide (HY-B0217) 的药代动力学特性,具有明显较长的消除半衰期 (t1/2β) (11.1 vs 0.8 h),更高的绝对生物利用度 (F) (87.4% vs 5.7%),以及更高的最大血浆浓度 (Cmax) (20.7 vs 1.0 mg/L)[1]。 |
| Name | STAT3-IN-17 |
| CAS | 1245814-52-1 |
| Formula | C11H6F3N3O3S |
| Molar Mass | 317.24 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Lü Z, et al. Structure-Activity Study of Nitazoxanide Derivatives as Novel STAT3 Pathway Inhibitors. ACS Med Chem Lett. 2021 Apr 1;12(5):696-703. |