Product IntroductionBioactivity英文名:
SC144 hydrochloride描述: SC144 hydrochloride 是首创的口服活性gp130 (IL6-beta)抑制剂。SC144 hydrochloride 结合 gp130,诱导 gp130 磷酸化(S782) 和去糖基化,消除 Stat3 磷酸化和核易位,进而抑制下游靶基因的表达。SC144 hydrochloride 对 gp130 配体触发的信号转导显示有效的抑制作用。SC144 hydrochloride 诱导人卵巢癌细胞凋亡。
体外活性: SC144 inhibits cell growth in a panel of human ovarian cancer cell lines with IC 50 s in a submicromolar range (IC 50 =OVCAR-8, OVCAR-5, OVCAR-3= 0.72, 0.49, 0.95 μM) [1]. The potency of SC144 against NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC 50 =0.43 μM) and HEY (Cisplatin-resistant, IC 50 =0.88 μM) demonstrates an ability to overcome drug resistance in ovarian cancer [1]. SC144 (2 μM; 24 hours) causes significantly more apoptosis in OVCAR-8 and Caov-3 than normal kidney epithelial and normal endometrial cells [1]. SC144 (0.5-2 μM; 0-6 hours) substantially increases the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cells in a time- and dose-dependent manner [1]. SC144 is cytotoxic to ovarian cancer cells via a mechanism involving the inhibition of gp130 activity, leading to the inactivation of Akt and Stat3 as well as the suppression of Stat3-regulated gene expression. As are result, SC144 treatment eventually causes cell-cycle arrest, anti-angiogenesis, and apoptosis [1]. Apoptosis Analysis [1] Cell Line: OVCAR-8 and Caov-3 cells Concentration: 2 μM Incubation Time: 24 hours Result: Significantly caused cell death in OVCAR-8 and Caov-3 cells. Western Blot Analysis [1] Cell Line: OVCAR-8, Caov-3 cells Concentration: 0.5-2 μM Incubation Time: 0-6 hours Result: Substantially increased the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cellsin a time- and dose-dependent manner.
体内活性: SC144 (10 mg/kg; i.p.; daily for 58 days) delays tumor growth in human ovariancancer xenografts [1]. SC144 (100 mg/kg; p.o.; daily for 35 days) treatment shows the average tumor volume in mice 82% smaller than that in the control group [1]. Animal Model: Athymic mice (human ovarian cancer xenograft) [1] Dosage: I.p; daily for 58 days Administration: 10 mg/kg Result: Significantly inhibited tumor growth by about 73%.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
关键字:
SC144 Hydrochloride |
SC-144 Hydrochloride |
SC-144 hydrochloride |
SC144 hydrochloride |
SC 144 Hydrochloride