| 中文名称: | SC144 hydrochloride | ||||
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| 英文名称: | SC144 hydrochloride | ||||
| 别名: | SC 144 hydrochloride;2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride;SC-144 hydrochloride | ||||
| CAS No: | 917497-70-2 | 分子式: | C16H12ClFN6O | 分子量: | 358.76 |
| CAS No: | 917497-70-2 | ||||
| 分子式: | C16H12ClFN6O | ||||
| 分子量: | 358.76 | ||||
基本信息
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产品编号： |
S10702 |
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产品名称： |
SC144 hydrochloride |
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CAS: |
917497-70-2 |
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： |
358.76 |
-20℃ |
1个月 |
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化学名： |
2-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide-2-pyrazinecarboxylic acid hydrochloride |
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Solubility (25°C)： |
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体外:
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DMSO |
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Ethanol |
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Water |
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体内(现配现用): |
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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 |
2.7874mL |
13.9369mL |
27.8738mL |
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5mM |
0.5575mL |
2.7874mL |
5.5748mL |
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10mM |
0.2787mL |
1.3937mL |
2.7874mL |
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。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。 |
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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: |
I.p;daily for 58 days |
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Administration: |
10mg/kg |
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Result: |
Significantly inhibited tumor growth by about 73%. |
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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 )
