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917497-70-2

中文名称 CS-2091
英文名称 2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride
CAS 917497-70-2
分子式 C17H12ClFN6O3
分子量 402.767
MOL 文件 917497-70-2.mol
917497-70-2 结构式 917497-70-2 结构式

基本信息

中文别名
N'-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪-2-甲酰肼盐酸盐
英文别名
CS-2091
SC144 HCl
SC144 hydrochloride
N'-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide
N’-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide Hydrochloride
2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride
2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl) 2-pyrazinecarboxylic acid hydrazide hydrochloride
所属类别
生物化工:激动剂抑制剂

物理化学性质

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

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H315-H319-H335
危险品标志Xi
危险类别码36/37/38
安全说明26-36/39
WGK Germany3
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
2024/04/30HY-15614ACS-2091
SC144 hydrochloride
917497-70-25mg900元
2024/04/30HY-15614ACS-2091
SC144 hydrochloride
917497-70-210mM * 1mLin DMSO990元
2024/04/30HY-15614ACS-2091
SC144 hydrochloride
917497-70-210mg1300元

常见问题列表

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。
靶点

IL6-beta

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: I.p; daily for 58 days
Administration: 10 mg/kg
Result: Significantly inhibited tumor growth by about 73%.
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