CS-2091
| 中文名称 | CS-2091 |
|---|---|
| 中文同义词 | N'-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪-2-甲酰肼盐酸盐;化合物 SC144 HYDROCHLORIDE;SC144盐酸盐 |
| 英文名称 | 2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride |
| 英文同义词 | 2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride;SC144 hydrochloride;SC144 HCl;2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl) 2-pyrazinecarboxylic acid hydrazide hydrochloride;N'-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide;CS-2091;N’-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide Hydrochloride |
| CAS号 | 917497-70-2 |
| 分子式 | C17H12ClFN6O3 |
| 分子量 | 402.7669832 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 917497-70-2.mol |
| 结构式 |  |
CS-2091 性质
| 熔点 | 282 °C (decomp)(Solv: methanol (67-56-1)) |
|---|---|
| 储存条件 | -20°C |
| 溶解度 | DMSO：可溶5mg/mL，澄清（加热） |
| 形态 | 粉末 |
| 颜色 | 白色至浅棕色 |
|
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: | I.p; daily for 58 days |
| Administration: | 10 mg/kg |
| Result: | Significantly inhibited tumor growth by about 73%. |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-15614A | CS-2091 SC144 hydrochloride | 917497-70-2 | 5mg | 900元 |
| 2024/04/30 | HY-15614A | CS-2091 SC144 hydrochloride | 917497-70-2 | 10mM * 1mLin DMSO | 990元 |