| 中文名称: | A-1210477 | ||||
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| 英文名称: | A-1210477 | ||||
| 别名: | 7-(1,3-Dimethyl-5-((4-(4-(methylsulfonyl)piperazin-1-yl)phenoxy)methyl)-1H-pyrazol-4-yl)-1-(2-morpholinoethyl)-3-(3-(naphthalen-1-yloxy)propyl)-1H-indole-2-carboxylic acid;7-[5-[[4-[4-[(Dimethylamino)sulfonyl]-1-piperazinyl]phenoxy]methyl]-1,3-dimethyl-1H-pyrazol-4-yl]-1-[2-(4-morpholinyl)ethyl]-3-[3-(1-naphthalenyloxy)propyl]-1H-indole-2-carboxylic acid | ||||
| CAS No: | 1668553-26-1 | 分子式: | C46H55N7O7S | 分子量: | 850.04 |
| CAS No: | 1668553-26-1 | ||||
| 分子式: | C46H55N7O7S | ||||
| 分子量: | 850.04 | ||||
基本信息
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产品编号：A11275 |
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产品名称：A-1210477 |
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CAS: |
1668553-26-1 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
850.04 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
6mg/mL warmed with 50ºC water bath (7.05mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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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 |
1.1764mL |
5.8821mL |
11.7642mL |
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5mM |
0.2353mL |
1.1764mL |
2.3528mL |
生物活性
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产品描述 |
一种有效，选择性的 MCL-1 抑制剂，Ki 值为 0.45 nM。 |
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靶点/IC50 |
Mcl-1 0.45nM (Ki) |
Bcl-2 132nM (Ki) |
Bfl-1 660nM (Ki) |
Bcl-W 2280nM (Ki) |
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Apoptosis |
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体外研究 |
A-1210477 (10μM) reduces the amount of BIM co-immunoprecipitated with MCL-1 antibody, and triggers MCL-1 elevation in a variety of cancer cell lines, including the breast cancer cell line HCC-1806. A-1210477 inhibits MCL-1-NOXA interactions with an IC50 of approximately 1μM, while having no effect on BCL-2-BIM or BCL-XL-BCL-XS interactions. The NSCLC cell lines H2110 and H23 are sensitive to A-1210477 with cell viability IC50<10μM, confirming that A-1210477 can kill MCL-1-dependent cell lines. |
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推荐实验方法(仅供参考)
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激酶实验： |
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TR-FRET-binding affinity assays are performed for BCL-2, BCL-XL, and MCL-1 in 4.52mM monobasic potassium phosphate,15.48mM dibasic potassium phosphate, 1mM sodium EDTA,0.05% Pluronic F-68 detergent, 50mM sodium chloride, and 1mM DTT (pH 7.5) for BCL-XL.6 For MCL-1 assays, GST-tagged MCL-1 (1nM) is mixed with 100nM f-Bak, 1 nM Tb-labeled antiGST antibody, and compound at room temperature (RT) for 60 min. Fluorescence is measured on an Envision plate reader using a 340/35nm excitation filter and 520/525 (f-Bak) and 495/510nm (Tb-labeled anti-GST antibody) emission filters. |
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细胞实验: |
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Adherent cell lines are seeded at 50 000 cells per well in 96-well plates and treated for 48h with compounds diluted in halflog steps starting at 30μM and ending at 0.001μM. Multiple myeloma cell lines are seeded at 15 000-20 000 cells per well and treated similarly. Effects on proliferation and viability are determined using CellTiter-Glo reagent from Promega according to the manufacturer's instructions. IC50 values are determined by non-linear regression analysis of the concentration response data. |
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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 )
