917497-70-2 | CS-2091
英文名称
2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride
分子式
C17H12ClFN6O3
分子量
402.77
结构式
中文别名
英文别名
| 属性 | 值 |
|---|---|
| 形态 | 粉末 |
| 熔点 | 282 °C (decomp)(Solv: methanol (67-56-1)) |
| 颜色 | 白色至浅棕色 |
| 溶解度 | DMSO：可溶5mg/mL，澄清（加热） |
| 储存条件 | -20°C |
| 属性 | 值 |
|---|---|
| 警示词 | 警告 |
| WGK Germany | 3 |
| 安全说明 | 26-36/39 |
| 防范说明 | P261-P305+P351+P338 |
| 危险品标志 | Xi |
| 危险性描述 | H315-H319-H335 |
| 危险类别码 | 36/37/38 |
| 危险性符号(GHS) | GHS07 |
| 标题 | 内容 |
|---|---|
| CS-2091价格(试剂级) | 报价日期 产品编号 产品名称 CAS号 包装 价格 2025/05/22 HY-15614A CS-2091 SC144 hydrochloride 917497-70-2 5mg 900元 2025/05/22 HY-15614A CS-2091 SC144 hydrochloride 917497-70-2 10mM * 1mLin DMSO 990元 2025/05/22 HY-15614A CS-2091 SC144 hydrochloride 917497-70-2 10mg 1300元 |
| 标题 | 内容 |
|---|---|
| 靶点 | IL6-beta |
| 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: I.p; daily for 58 days Administration: 10 mg/kg Result: Significantly inhibited tumor growth by about 73%. |
| 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. |
| 生物活性 | 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，进一步抑制下游靶基因的表达。SC144 hydrochloride 对 gp130 配体触发的信号转导有明显的抑制作用。SC144 hydrochloride 诱导人卵巢癌细胞凋亡。 |