中文名 | SC144 |
英文名 | SC144 |
别名 | GP130抑制剂(SC144) 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪羧酸酰肼 吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼 N'-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪-2-甲酰肼 吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼 1级 |
英文别名 | SC144 SC144 SC-144 SC 144 CS-805 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide Pyrazinecarboxylic acid 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide 2-Pyrazinecarboxylic acid, 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide |
CAS | 895158-95-9 |
化学式 | C16H11FN6O |
分子量 | 322.3 |
密度 | 1.53±0.1 g/cm3(Predicted) |
酸度系数 | 8.87±0.43(Predicted) |
存储条件 | -20℃ |
体外研究 | 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). The potency of SC144 toward NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC 50 =0.43 μM) and HEY (Cisplatin-resistant, IC 50 =0.88 μM) suggests an ability to overcome drug resistance in ovarian cancer. SC144 (2 μM; 24 hours) causes significantly more apoptosis in OVCAR-8 and Caov-3 than normal kidney epithelial and normal endometrial cells. 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. 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. Apoptosis Analysis 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 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. |
体内研究 | SC144 (10 mg/kg; i.p.; daily for 58 days) suppresses tumor growth in human ovariancancer xenografts. 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. Animal Model: Athymic mice (human ovarian cancer xenograft) Dosage: 10 mg/kg Administration: I.p; daily for 58 days Result: Significantly inhibited tumor growth by about 73%. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.103 ml | 15.513 ml | 31.027 ml |
5 mM | 0.621 ml | 3.103 ml | 6.205 ml |
10 mM | 0.31 ml | 1.551 ml | 3.103 ml |
5 mM | 0.062 ml | 0.31 ml | 0.621 ml |
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