| 中文名称: | ZLDI-8 | ||||
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| 英文名称: | ZLDI-8 | ||||
| 别名: | ZLDI-8;BDBM50031904;5-({1-[2-(2,4-dimethylphenoxy)ethyl]-2-methyl-1H-indol-3-yl}methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione;5-[[1-[2-(2,4-Dimethylphenoxy)ethyl]-2-methylindol-3-yl]methylidene]-2-sulfanylidene-1,3-diazinane-4 | ||||
| CAS No: | 667880-38-8 | 分子式: | C24H23N3O3S | 分子量: | 433.52 |
| CAS No: | 667880-38-8 | ||||
| 分子式: | C24H23N3O3S | ||||
| 分子量: | 433.52 | ||||
基本信息
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产品编号： |
Z10036 |
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产品名称： |
ZLDI-8 |
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CAS: |
667880-38-8 |
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 |
433.52 |
-20℃ |
1个月 |
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化学名： |
5-[[1-[2-(2,4-Dimethylphenoxy)ethyl]-2-methylindol-3-yl]methylidene]-2-sulfanylidene-1,3-diazinane-4 |
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Solubility (25°C)： |
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体外:
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DMSO |
62.5 mg/mL (144.17mM; Need ultrasonic) |
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Water |
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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 |
2.3067mL |
11.5335mL |
23.0670mL |
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5mM |
0.4613mL |
2.3067mL |
4.6134mL |
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10mM |
0.2307mL |
1.1533mL |
2.3067mL |
生物活性
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产品描述 |
一种 Notch 活化/裂解酶 ADAM-17 抑制剂，可抑制 Notch 蛋白的裂解，并降低促存活/抗凋亡和上皮-间质转化相关蛋白的表达。 |
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靶点 |
ADAM-17 IC50: 31.6μM (Tyrosine phosphatase)Ki: 26.22μM (Tyrosine phosphatase) |
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体外研究 |
ZLDI-8 (0.03-30 μM; 6-72 hours; MHCC97-H cells) treatment reduces cell viability in a time- and dose-dependent manner. ZLDI-8 (1-10 μM; 6-72 hours; MHCC97-H cells) significantly decreases the level of NICD and the accumulation of NICD in the nucleus. ZLDI-8 could also reduce the expression of pro-survival/anti-apoptosis regulators, Survivin and cIAP1/2. And also increases the expression of epithelial marker E-Cadherin and reduced mesenchymal markers N-Cadherin and Vimentin.ZLDI-8 enhances chemotherapy effects on tumor cell proliferation blockage, induction of apoptosis and cell-cycle arrest by inhibiting Notch pathway and blocking chemical resistance. Cell Viability Assay
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Cell Line: |
MHCC97-H cells |
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Concentration: |
0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM |
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Incubation Time: |
6 hours, 12 hours, 24 hours, 48 hours, 72 hours |
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Result: |
Emerged cytotoxic effect on MHCC97-H cells in a time- and dose-dependent manner. |
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Western Blot Analysis |
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Cell Line: |
MHCC97-H cells |
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Concentration: |
1μM, 3μM, 10μM |
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Incubation Time: |
6 hours, 12 hours, 24 hours, 48 hours, 72 hours |
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Result: |
Significantly decreased the level of NICD and the accumulation of NICD in the nucleus. Also reduced the expression of pro-survival/anti-apoptosis regulators, Survivin and cIAP1/2 |
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体内研究 |
ZLDI-8 (0.2-2 mg/kg; intraperitoneal injection; every two days; for 20 days; nude mice) treatment enhances the effect of Sorafenib on inhibiting tumor growth in nude HCC-bearing mice model |
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Animal Model: |
Nude mice with MHCC-97H cells |
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Dosage: |
2 mg/kg, 1 mg/kg, 500μg/kg, or 200μg/kg |
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Administration: |
Intraperitoneal injection; every two days; for 20 days |
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Result: |
Inhibited tumor growth in nude HCC-bearing mice model. |
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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 )
