CS-2091
- CAS号:917497-70-2
- 英文名:2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride
- 中文名:CS-2091
- CBNumber:CB72750597
- 分子式:C17H12ClFN6O3
- 分子量:402.7669832
- MOL File:917497-70-2.mol
- 熔点 :282 °C (decomp)(Solv: methanol (67-56-1))
- 储存条件 :-20°C
- 溶解度 :DMSO: soluble5mg/mL, clear (warmed)
- 形态 :powder
- 颜色 :white to light brown
CS-2091性质、用途与生产工艺
- 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。
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靶点
IL6-beta
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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%.
- 更新日期:2025/02/08
- 产品编号:HY-15614A
- 产品名称:CS-2091 SC144 hydrochloride
- CAS编号:917497-70-2
- 包装:5mg
- 价格:900元
- 更新日期:2025/02/08
- 产品编号:HY-15614A
- 产品名称:CS-2091 SC144 hydrochloride
- CAS编号:917497-70-2
- 包装:10mM * 1mLin DMSO
- 价格:990元
- 公司名称:TOCRIS-US
- 联系电话:--
- 电子邮件:customerservice@tocris.co.uk
- 国家:英国
- 产品数:5726
- 优势度:77