吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼
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- CAS号:
- 895158-95-9
- 英文名:
- SC 144
- 英文别名:
- SC144;SC-144;SC 144;CS-805;SC 144; SC144;SC144;SC-144;SC 144;2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide;N'-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide;N'-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)-2-pyrazinecarbohydrazide;Pyrazinecarboxylic acid 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide
- 中文名:
- 吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼
- 中文别名:
- GP130抑制剂(SC144);SC144,GP130 (IL6-BETA) 抑制剂;2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪羧酸酰肼;吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼;N'-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪-2-甲酰肼;N'-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪-2-甲酰肼;吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼 1级
- CBNumber:
- CB72666896
- 分子式:
- C16H11FN6O
- 分子量:
- 322.3
- MOL File:
- 895158-95-9.mol
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吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼化学性质
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密度:
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1.53±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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insoluble in EtOH; insoluble in H2O; ≥16.1 mg/mL in DMSO
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形态:
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solid
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酸度系数(pKa):
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8.87±0.43(Predicted)
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颜色:
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Light yellow to yellow
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吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼性质、用途与生产工艺
SC144是一种口服活性小分子gp130抑制剂。
SC144 是首创的口服活性 gp130 (IL6-beta) 抑制剂。SC144 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 对 gp130 配体触发的信号转导有明显的抑制作用。SC144 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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10 mg/kg
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Administration:
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I.p; daily for 58 days
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Result:
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Significantly inhibited tumor growth by about 73%.
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吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼
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-15614 | SC144 | | 1 mg | 250元 |
| 2024/04/30 | HY-15614 | 吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼
SC144 | 895158-95-9 | 5mg | 550元 |
吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼
生产厂家
895158-95-9, 吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼 相关搜索:
- Inhibitors
- 药靶配体
- 细胞生物学试剂
- 小分子抑制剂，天然产物
- C16H11FN6O
- N'-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪-2-甲酰肼
- SC144,GP130 (IL6-BETA) 抑制剂
- N'-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪-2-甲酰肼
- 吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼 1级
- 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)吡嗪羧酸酰肼
- GP130抑制剂(SC144)
- 吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼
- 895158-95-9
- N'-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide
- SC144
- N'-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)-2-pyrazinecarbohydrazide
- SC144;SC-144;SC 144
- CS-805
- SC 144; SC144
- Pyrazinecarboxylic acid 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide
- SC-144
- SC 144
- 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide
- 2-Pyrazinecarboxylic acid, 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide