CS-2091
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- CAS号:
- 917497-70-2
- 英文名:
- 2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride
- 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
- 中文名:
- CS-2091
- 中文别名:
- SC144盐酸盐;化合物 SC144 HYDROCHLORIDE;N'-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪-2-甲酰肼盐酸盐
- CBNumber:
- CB72750597
- 分子式:
- C17H12ClFN6O3
- 分子量:
- 402.7669832
- MOL File:
- 917497-70-2.mol
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CS-2091化学性质
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熔点:
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282 °C (decomp)(Solv: methanol (67-56-1))
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储存条件:
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-20°C
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溶解度:
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DMSO: soluble5mg/mL, clear (warmed)
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形态:
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powder
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颜色:
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white to light brown
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CS-2091性质、用途与生产工艺
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。
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
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Cell Line:
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OVCAR-8 and Caov-3 cells
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Concentration:
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2 μM
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Incubation Time:
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24 hours
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Result:
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Significantly caused cell death in OVCAR-8 and Caov-3 cells.
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Western Blot Analysis
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Cell Line:
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OVCAR-8, Caov-3 cells
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Concentration:
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0.5-2 μM
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Incubation Time:
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0-6 hours
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Result:
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Substantially increased the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cellsin a time- and dose-dependent manner.
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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.
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Animal Model:
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Athymic mice (human ovarian cancer xenograft)
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Dosage:
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I.p; daily for 58 days
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Administration:
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10 mg/kg
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Result:
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Significantly inhibited tumor growth by about 73%.
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CS-2091
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
917497-70-2, CS-2091 相关搜索:
- 药靶配体
- C16H12ClFN6O
- SC144盐酸盐
- 化合物 SC144 HYDROCHLORIDE
- N'-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪-2-甲酰肼盐酸盐
- 917497-70-2
- N’-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide Hydrochloride
- CS-2091
- N'-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide
- 2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl) 2-pyrazinecarboxylic acid hydrazide hydrochloride
- SC144 HCl
- SC144 hydrochloride
- 2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride