| 中文名称: | SC144 | ||||
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| 英文名称: | SC144 | ||||
| 别名: | 吡嗪羧酸 2-(7-氟吡咯并[1,2-A]喹喔啉-4-基)酰肼 N'-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)-2-pyrazinecarbohydrazi De;SC144;Sc-144 | ||||
| CAS No: | 895158-95-9 | 分子式: | C16H11FN6O | 分子量: | 322.3 |
| CAS No: | 895158-95-9 | ||||
| 分子式: | C16H11FN6O | ||||
| 分子量: | 322.3 | ||||
基本信息
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产品编号： |
S10688 |
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产品名称： |
SC144 |
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CAS: |
895158-95-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
322.30 |
-20℃ |
1个月 |
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化学名： |
N'-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)-2-pyrazinecarbohydrazi De |
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Solubility (25°C)： |
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体外:
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DMSO |
64mg/mL (198.57mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内(现配现用): |
30% propylene glycol,5% Tween 80,65% D5W |
30mg/mL |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
3.1027mL |
15.5135mL |
31.0270mL |
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5mM |
0.6205mL |
3.1027mL |
6.2054mL |
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10mM |
0.3103mL |
1.5513mL |
3.1027mL |
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50mM |
0.0621mL |
0.3103mL |
0.6205mL |
生物活性
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产品描述 |
是首创的口服活性gp130 (IL6-beta)抑制剂。 |
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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 IC50s in a submicromolar range (IC50=OVCAR-8,OVCAR-5,OVCAR-3=0.72,0.49,0.95μM).The potency of SC144 toward NCI/ADR-RES (Paclitaxel-and Doxorubicin-resistant,IC50=0.43μM) and HEY (Cisplatinresistant,IC50=0.88μM) suggests an ability to overcome drug resistance in ovarian cancer.SC144 (2μM;24 hours) causes significantly more apoptosis in OVCAR-8 and Caov-3 than normal kidney epithelial and normal endometrial cells.SC144 (0.5-2μM;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: |
OVCAR-8 and Caov-3 cells |
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Concentration: |
2μM |
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Incubation Time: |
24 hours |
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Result: |
Significantly caused cell death in OVCAR-8 and Caov-3 cells. |
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Western Blot Analysis |
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Cell Line: |
OVCAR-8,Caov-3 cells |
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Concentration: |
0.5-2μM |
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Incubation Time: |
0-6 hours |
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Result: |
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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体内研究 |
SC144 (10mg/kg;i.p.;daily for 58 days) suppresses tumor growth in human ovariancancer xenografts.SC144 (100mg/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: |
Athymic mice (human ovarian cancer xenograft) |
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Dosage: |
10mg/kg |
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Administration: |
I.p;daily for 58 days |
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Result: |
Significantly inhibited tumor growth by about 73%. |
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推荐实验方法(仅供参考)
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细胞实验: |
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细胞系 |
OVCAR-8,OVCAR-5,OVCAR-3,Caov-3,SKOV-3,HEY NCI/ADR-RES |
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浓度 |
~10μM |
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处理时间 |
96小时 |
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方法 |
MTT检测 |
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动物实验: |
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动物模型 |
人卵巢癌OVCAR-8异种移植 |
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剂量 |
10毫克/千克,每天 |
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给药处理 |
腹腔注射或口服 |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
