| 中文名称: | RU-SKI 43 hydrochloride | ||||
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| 英文名称: | RU-SKI 43 hydrochloride | ||||
| 别名: | RU-SKI 43（盐酸盐） 1-[6,7-dihydro-4-[(3-methylphenoxy)methyl]thieno[3,2-c]pyridin-5(4H)-yl]-2-[(2-methylbutyl)amino]-ethanone, monohydrochloride | ||||
| CAS No: | 1782573-67-4 | 分子式: | C22H31ClN2O2S | 分子量: | 423.012 |
| CAS No: | 1782573-67-4 | ||||
| 分子式: | C22H31ClN2O2S | ||||
| 分子量: | 423.012 | ||||
基本信息
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产品编号： |
R10445 |
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产品名称： |
RU-SKI 43 hydrochloride |
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CAS: |
1782573-67-4 |
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 |
423.01 |
-20℃ |
1个月 |
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化学名： |
1-[6,7-dihydro-4-[(3-methylphenoxy)methyl]thieno[3,2-c]pyridin-5(4H)-yl]-2-[(2-methylbutyl)amino]-ethanone, monohydrochloride |
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Solubility (25°C)： |
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体外:
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DMSO |
≥ 51 mg/mL (120.56mM) |
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Water |
2.5 mg/mL (5.91mM; Need ultrasonic) |
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Ethanol |
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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 |
2.3640mL |
11.8201mL |
23.6401mL |
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5mM |
0.4728mL |
2.3640mL |
4.7280mL |
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10mM |
0.2364mL |
1.1820mL |
2.3640mL |
生物活性
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产品描述 |
一种有效的选择性刺猬酰基转移酶 (Hhat) 抑制剂，IC50 为 850nM。RU-SKI 43 hydrochloride 通过独立于平滑化的非规范信号传导降低 Gli-1 激活，并抑制 Akt 和 mTOR 通路活性。RU-SKI 43 hydrochloride 具有抗癌活性。 |
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靶点 |
IC50: 850nM (Hhat) |
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体外研究 |
RU-SKI 43 hydrochloride (10μM; for 6 days) strongly decreases cell proliferation (83% in AsPC-1 cells) in AsPC-1 and Panc-1 cells . RU-SKI 43 hydrochloride (10 or 20μM; 5 hours) causes dose-dependent inhibition of Shh palmitoylation following only 5 hours. RU-SKI 43 hydrochloride (10μM; for 72 hours) causes a 40% decrease in Gli-1 levels in AsPC-1 cells. RU-SKI 43 hydrochloride (10μM; 48 hours) results in decreased phosphorylation (47-67%) of four proteins in the Akt pathway, including Akt (phosphorylation at both Thr307 and Ser473), PRAS40, Bad and GSK-3β. RU-SKI 43 treatment also decreases phosphorylation of mTOR and S6, members of the mTOR signaling pathway. RU-SKI 43 hydrochloride behaves as an uncompetitive inhibitor (Ki=7.4μM) with respect to Shh, and as a noncompetitive inhibitor (Ki=6.9μM) with respect to 125I-iodo-palmitoylCoA . Cell Proliferation Assay |
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Cell Line: |
AsPC-1 and Panc-1 pancreatic cancer cells |
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Concentration: |
10μM |
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Incubation Time: |
For 6 days (drugs were replenished every 48 hours) |
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Result: |
Strongly decreased cell proliferation (83% in AsPC-1 cells). |
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Western Blot Analysis |
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Cell Line: |
COS-1 cells expressing HA-Hhat and Shh |
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Concentration: |
10 or 20μM |
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Incubation Time: |
5 hours |
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Result: |
Caused dose-dependent inhibition of Shh palmitoylation following only 5 hours. |
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体内研究 |
RU-SKI 43 hydrochloride has a t1/2 of 17 min in mouse plasma after IV administration. |
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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 )
