吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼
| 中文名称 | 吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼 |
|---|---|
| 中文同义词 | 吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼;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 1级;N'-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪-2-甲酰肼;SC144,GP130 (IL6-BETA) 抑制剂;N'-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪-2-甲酰肼 |
| 英文名称 | SC 144 |
| 英文同义词 | 2-Pyrazinecarboxylic acid, 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide;2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide;SC 144;SC-144;Pyrazinecarboxylic acid 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide;SC 144; SC144;CS-805;SC144;SC-144;SC 144 |
| CAS号 | 895158-95-9 |
| 分子式 | C16H11FN6O |
| 分子量 | 322.3 |
| EINECS号 | |
| 相关类别 | 小分子抑制剂，天然产物;细胞生物学试剂;Inhibitors |
| Mol文件 | 895158-95-9.mol |
| 结构式 | ![吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼 结构式](CAS/20150408/GIF/895158-95-9.gif) |
吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼 性质
| 密度 | 1.53±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 不溶于乙醇；不溶于水； DMSO 中≥16.1 mg/mL |
| 形态 | 固体 |
| 酸度系数(pKa) | 8.87±0.43(Predicted) |
| 颜色 | 浅黄至黄色 |
SC144是一种口服活性小分子gp130抑制剂。
SC144 是首创的口服活性 gp130 (IL6-beta) 抑制剂。SC144 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，进一步抑制下游靶基因的表达。SC144 对 gp130 配体触发的信号转导有明显的抑制作用。SC144 诱导人卵巢癌细胞凋亡。|
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%. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/11/08 | HY-15614 | SC144 | 1 mg | 250元 | |
| 2024/11/08 | HY-15614 | 吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼 SC144 | 895158-95-9 | 5mg | 550元 |