895158-95-9
基本信息
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
SC 144
SC-144
CS-805
SC 144
SC144
SC144
SC-144
SC 144
2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide
N'-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)-2-pyrazinecarbohydrazide
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
物理化学性质
| 密度 | 1.53±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C储存 |
| 溶解度 | insoluble in EtOH; insoluble in H2O; ≥16.1 mg/mL in DMSO |
| 酸度系数(pKa) | 8.87±0.43(Predicted) |
| 形态 | 固体 |
| 颜色 | Light yellow to yellow |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319-H335 |
| 防范说明 | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
常见问题列表
SC144是一种口服活性小分子gp130抑制剂。
|
IL6-beta
|
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. |
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%. |