中文名称: | Stauprimide | ||||
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英文名称: | Stauprimide | ||||
别名: | 顺式1-苄基-4-甲基-3-甲氨基-哌啶盐酸盐;抑胃酶氨酰u丙基亚胺;抑胃酶氨酰U丙基亚胺 N-[(9S,10R,11R,13R)-2,3,10,11,12,13-Hexahydro-10-methoxy-9-methyl-1,3-dioxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl]-N-methylbenzamide | ||||
CAS No: | 154589-96-5 | 分子式: | C35H28N4O5 | 分子量: | 584.62 |
CAS No: | 154589-96-5 | ||||
分子式: | C35H28N4O5 | ||||
分子量: | 584.62 |
基本信息
产品编号:S10730 |
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产品名称:Stauprimide |
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CAS: |
154589-96-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
-80℃(氮气储存) |
六个月 |
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分子量 |
584.62 |
-20℃(氮气储存) |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
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。 |
生物活性
产品描述 |
一种促进胚胎干细胞 (ESC) 分化的星形孢菌素类似物。Stauprimide 与 MYC 转录因子 NME2 结合并阻断其在 ESC 中的核定位,导致 MYC 转录的下调, 是一种非广谱抑制剂。 |
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靶点/IC50 |
c-Myc; Autophagy |
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体外研究 |
Stauprimide (10μM; 6 hours) suppresses MYC transcription in the majority of cell lines tested with an EC50 range of 30nM-8 μM, and decreases MYC levels between 15% to over 90%.Stauprimide (2-8μM; 24-72 hours) down-regulates MYC leads to the inhibition of cell proliferation in vitro with an IC50 of 780nM in RXF 393 cells.Stauprimide (5μM; 3 hours) suppresses MYC Transcription by decreasing NME2 Nuclear Translocation.Stauprimide (4-10μM; 6 hours) acts with different EC50s and with different degrees of maximal MYC mRNA down-regulation in different cell lines. Cell Proliferation Assay |
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Cell Line: |
Renal cancer cell line RXF 393 cells |
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Concentration: |
2μM, 4μM, 8μM |
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Incubation Time: |
24 hours, 48 hours, 72 hours |
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Result: |
Inhibited cell proliferation at concentrations of 2-8μM. |
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Western Blot Analysis |
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Cell Line: |
Renal cancer cell line RXF 393 cells and CAKI-1 cells |
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Concentration: |
5μM |
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Incubation Time: |
3 hours |
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Result: |
Decreased nuclear localized NME2. |
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RT-PCR |
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Cell Line: |
CA46 cells; Ramos cells; RXF393 cells; TK10 cells; KG1A cells; CAKI-1 cells |
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Concentration: |
4μM, 6μM, 8μM, 10μM |
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Incubation Time: |
6 hours |
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Result: |
Suppressed MYC transcription in KG1A cells with an EC50 of 400±50nM and a suppression of 90%; CA46 cells were resistant to stauprimide. |
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体内研究 |
Stauprimide (oral administration; 50mg/kg; once daily; 30 days, 55 days) blocks tumor growth,reduces MYC protein levels in xenograft mouse with RXF 393 or CAKI-1 cells and inhibits MYC transcription in the RXF 393 tumor. |
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Animal Model: |
Xenograft tumor models with RXF 393 and CAKI-1 cells in NOD/SCID mice |
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Dosage: |
50mg/kg |
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Administration: |
Oral administration; 50mg/kg; once daily;30 days,55 days |
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Result: |
Blocked tumor growth in mice injected with either RXF 393 or CAKI-1 cells during the dosing periods. |
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 )