中文名称: | 3CAI | ||||
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英文名称: | 3CAI | ||||
别名: | 2-氯-1-(1H-吲哚-3-基)乙酮 2-Chloro-1-(1H-indol-3-yl)ethanone | ||||
CAS No: | 28755-03-5 | 分子式: | C10H8ClNO | 分子量: | 193.63 |
CAS No: | 28755-03-5 | ||||
分子式: | C10H8ClNO | ||||
分子量: | 193.63 |
基本信息
产品编号: |
C70166 |
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产品名称: |
3CAI |
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CAS: |
28755-03-5 |
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: |
193.63 |
-20℃ |
1个月 |
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化学名: |
2-Chloro-1-(1H-indol-3-yl)ethanone |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
5.1645mL |
25.8224mL |
51.6449mL |
5mM |
1.0329mL |
5.1645mL |
10.3290mL |
10mM |
0.5164mL |
2.5822mL |
5.1645mL |
生物活性
产品描述 |
一种有效的特异性AKT1和AKT2抑制剂。 |
靶点 |
Akt |
体外研究 |
3CAI is a potential inhibitor of AKT.Based on these screening data,the effect of 3CAI on the kinase activities of AKT1,MEK1,JNK1,ERK1 and TOPK is tested using in vitro kinase assays.The results show that 3CAI (1μM) suppresses only AKT1 kinase activity and the other kinases tested are not affected by 3CAI.3CAI is a much more potent AKT1 inhibitor than PI3K (60% inhibition at 1 vs 10μM,respectively).3CAI substantially suppresses AKT1 activity as well as AKT2 activity in a dose dependent manner.3CAI inhibits down-stream targets of AKT and induces apoptosis.AKT-mediated phosphorlyation site of mTOR (Ser2448) and GSK3β(Ser9) are substantially decreased by 3CAI in a time-dependent manner.Furthermore,proapoptotic marker proteins p53 and p21 are also upregulated by 3CAI after 12 or 24h of treatment.HCT116 and HT29 colon cancer cells are seeded on 6 cm dishes in 1% FBS/McCoy's 5A (HCT116) with 3CAI (4μM),I3C or the AKT inhibitor and then incubated for 4 days.Results show that the number of apoptotic cells is significantly increased by 3CAI in HCT116 and HT29 colon cancer cells compared with untreated control cells. |
体内研究 |
To examine the antitumor activity of 3CAI in vivo,HCT116 cancer cells are injected into the right flank of individual athymic nude mice.Mice are orally administered 3CAI at 20 or 30mg/kg,I3C at 100mg/kg,or vehicle 5 times a week for 21 days.Treatment of mice with 30mg/kg of 3CAI significantly suppresses HCT116 tumor growth by 50% relative to the vehicletreated group(p<0.05).Remarkably,mice seem to tolerate treatment with these doses of 3CAI without overt signs of toxicity or significant loss of body weight compared with vehicle-treated group.Expression of these AKT-target proteins is strongly suppressed by 30mg/kg of 3CAI in tumor tissues. |
推荐实验方法(仅供参考)
激酶实验: |
The kinase assay is performed.Briefly,the reaction is carried out in the presence of 10μCi of [γ-32P]ATP with each compound (e.g.,3CAI,0.5,1,2 and 4μM) in 40μL of reaction buffer containing 20mM HEPES (pH 7.4),10mM MgCl2,10mM MnCl2,and 1mM dithiothreitol.After incubation at room temperature for 30 min,the reaction is stopped by adding 10μL protein loading buffer and the mixture is separated by sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDSPAGE).The relative amounts of incorporated radioactivity are assessed by autoradiography. |
细胞实验: |
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HCT116 or HCT29 colon cancer cells are plated into 60-mm culture dishes (1×105 cells/dish) and incubated for 1 day in medium containing 10% FBS.The culture medium is then replaced with a 1% serum medium and cultured for 4 days with 3CAI (4μM),I3C or a commercial AKT inhibitor.The cells are collected by trypsinization and washed with phosphate buffered saline (PBS).The cells are resuspended in 200μL of binding buffer. Annexin V staining is accomplished. The cells are observed under a fluorescence microscope using a dual filter set for FITC and propidium iodide and then analyzed by flow cytometry. |
动物实验: |
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Mice Athymic mice [Cr:NIH(S),NIH Swiss nude,6-9 wk old] are divided into five groups:1) untreated vehicle group (n=15);2) 20mg 3CAI/kg of body weight (n=15),3) 30mg 3CAI/kg body weight (n=15);4) 100 mg I3C/kg of body weight (n=15);5) no cells and 30mg 3CAI/kg of body weight (n=15).HCT116 cells (3×106 cells/100μL) are suspended in serum free McCoy's 5A medium and inoculated subcutaneously into the right flank of each mouse.3CAI,I3C or vehicle is administered orally 5 times per week for 21 days.Tumor volume is calculated.Mice are monitored until tumors reach 1 cm3 total volume,at which time mice are euthanized and tumors are extracted. |
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 )