基本属性 生物活性靶点体外研究体内研究 用途与合成方法 CS-2091 价格(试剂级) 供应商 供应信息
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CS-2091

CS-2091

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号:917497-70-2
分子式:C17H12ClFN6O3
分子量:402.7669832
EINECS号:
Mol文件:917497-70-2.mol
CS-2091 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

CS-2091 用途与合成方法

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。

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%.

安全信息

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)

更新日期 产品编号 产品名称 CAS号 包装 价格
2025-02-08 HY-15614A CS-2091 917497-70-2 5mg 900
2025-02-08 HY-15614A CS-2091 917497-70-2 10mM * 1mLin DMSO 990

CS-2091供应商 更多

Sigma-Aldrich西格玛奥德里奇(上海)贸易有限公司
联系电话:021-61415566 800-8193336
产品介绍:
英文名称:SC144
CAS:917497-70-2
纯度:>=98% (HPLC)
包装信息:5mg, 25mg
备注:SML0763
上海一飞生物科技有限公司
联系电话:021-65675885 18964387627
产品介绍:
英文名称:SC 144 hydrochloride
CAS:917497-70-2
纯度:98%
包装信息:1mg;2mg;5mg
备注:试剂级
上海瀚香生物科技有限公司
联系电话:17754423994 17754423994
产品介绍:
英文名称:SC144 hydrochloride
CAS:917497-70-2
纯度:98% HPLC LCMS
包装信息:100mg;500mg;1g;5g;10g
备注:量大优惠,现货促销
北京索莱宝科技有限公司
联系电话:010-50973130 4009686088
产品介绍:
中文名称:SC144盐酸盐
CAS:917497-70-2
北京普西唐生物科技有限公司
联系电话:010-60605840 18892239720
产品介绍:
英文名称:SC144 hydrochloride
CAS:917497-70-2
纯度:98%
包装信息:5mg

最新发布供应信息

化合物 SC144 hydrochloride|T41260|TargetMol
TargetMol中国(陶术生物) 2025-02-28
aladdin 阿拉丁 S288107 SC 144 盐酸盐 917497-70-2 ≥98%(HPLC)
上海阿拉丁生化科技股份有限公司 2025-02-27