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（ 母液浓度为 40 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们客服联系。| 中文名称: | 罗米鲁曲 一键复制产品信息 | ||||
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| 英文名称: | Lomeguatrib | ||||
| 别名: | 罗米鲁曲 PaTrin-2 | ||||
| CAS No: | 192441-08-0 | 分子式: | C10H8BrN5Os | 分子量: | 326.17 |
| CAS No: | 192441-08-0 | ||||
| 分子式: | C10H8BrN5Os | ||||
| 分子量: | 326.17 | ||||
包装规格：
5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：
溶于DMSO（≥56mg/mL）
产品描述：
基本信息
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产品编号：L10388 |
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产品名称：Lomeguatrib |
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CAS: |
192441-08-0 |
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： |
326.17 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
65mg/mL (199.28mM) |
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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 |
3.0659mL |
15.3294mL |
30.6589mL |
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5mM |
0.6132mL |
3.0659mL |
6.1318mL |
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10mM |
0.3066mL |
1.5329mL |
3.0659mL |
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50mM |
0.0613mL |
0.3066mL |
0.6132mL |
生物活性
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产品描述 |
一种有效的 MGMT 抑制剂，在非细胞体系和 MCF-7 细胞体系中，IC50 值分别为 9nM 和∼6nM。 |
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靶点/IC50 |
O6-alkylguanine-DNA-alkyltransferas |
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5nM |
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体外研究 |
Lomeguatrib (Compound 10) is a O6-methylguanine methyltransferase (MGMT) inhibitor,with an IC50 of 9nM in cell-free assay and -6nM in MCF-7 cells.Lomeguatrib (10μM) substantially increases the growth inhibitory effects of temozolomide in MCF-7 cells (D60=10μM with Lomeguatrib vs 400μM without). |
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体内研究 |
Lomeguatrib (20mg/kg i.p.) completely inactivates MGMT within 2h,but shows no significant effect on tumor growth in MCF-7 xenografts. |
推荐实验方法(仅供参考)
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激酶实验： |
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Briefly,200μg of extracted cellular protein from HeLaS3 cells in 200μL of 70mM HEPES buffer (with 1mM dithiothreitol (DTT),5mM EDTA,pH 7.8) is incubated at 37℃ with a defined concentration of Lomeguatrib (added as a DMSO solution).After 30 min an excess of [3H]-methylated DNA (120 000 cpm) is added,and the incubation is continued for an additional 90 min.The reaction is stopped by the addition of 400μL TCA (13%),and the DNA is hydrolyzed by heating the reaction mixture for 30 min at 98℃.The precipitated protein is washed three times with 400-μL portions of 5% TCA,solubilized in 0.1N NaOH,and analyzed by liquid scintillation counting using the cocktail Rotiszint eco plus and a TRI-CARB.Enzyme activity is expressed as fmol of [3H]methyl transferred to TCA-insoluble protein material per mg of total cellular protein.Percent inhibition is calculated relative to untreated control samples.Each assay is repeated three times,and IC50 values are determined graphically from plots of percent inhibition vs inhibitor concentration. |
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细胞实验: |
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To determine toxicity,the MTT growth inhibition assay is employed.Cells (1000 per well) are plated into a 96-well plate and following a 24h attachment period,Lomeguatrib is added to the cells.After 2h incubation with Lomeguatrib (10μM) at 37℃,5% CO2,increasing doses of temozolomide or vehicle are added and the cells are incubated for a further 4-5 days.At the end of the exposure period,150μg MTT is added to each well and plates are incubated for 3h at 37℃,5% CO2.The media are removed and the formazan crystals formed in the viable cells are solubilised in 200μL DMSO.The absorbances at 540 and 690nm are determined using a ELISA plate reader and growth inhibition calculated as a percentage of the A540-A690 of untreated wells. |
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动物实验: |
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Mice To assess the ability of Lomeguatrib to sensitise human breast tumour xenografts to the tumour growth inhibitory effects of temozolomide,groups of at least six nude mice are treated as follows: the vehicle control group are given corn oil then 20% DMSO in PBS;the temozolomide only group are given corn oil then temozolomide (100mg/kg/day);the Lomeguatrib only group are given Lomeguatrib (20mg/kg/day) then DMSO in PBS,and the Lomeguatrib plus temozolomide group are given Lomeguatrib (20mg/kg/day) then temozolomide (100mg/kg/day).Drugs or vehicles are administered i.p.once daily for 5 days with a separation of 1h.Up to 10 and at least six animals are assigned to each group,and mean tumour volume is standardised across the groups at the start of the experiment:thus the control,Lomeguatrib, temozolomide and Lomeguatrib plus temozolomide groups had mean tumour volumes of 29.8±7.6 (range 19.0-38.7),33.2±14.7 (range 16.5-58.7),35.1±10.9 (range 20.9-52.4) and 30.3±10.0 (range 20.7-44.5) mm3,respectively. |
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保存条件：
-20℃
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
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 )
(2).jpg)
体内配方的制备方法: 取 50μLDMSO 母液，添加 300 μLPEG300 混匀澄清，再加 50μLTween80, 混匀澄清，再加 600μLSaline/PBS/ddH2O 混匀澄清
方案所需的各种助溶剂如： DMSO ， PEG300 / PEG400 ， Tween 80 ， SBE-β-CD ， 玉米油 等， 均可点击跳转或在网站搜索购买。
母液，添加 300 μLPEG300 混匀澄清，再加 50μLTween80, 混匀澄清，再加 600μLSaline/PBS/ddH2O 混匀澄清方案所需的各种助溶剂如： DMSO ， PEG300 / PEG400 ， Tween 80 ， SBE-β-CD ， 玉米油 等， 均可点击跳转或在网站搜索购买。
以上为“动物实验计算换算器”的使用方法举例，并不是具体某个试剂的配制，请根据您的实验动物和给药方式选择适当的溶解方案。
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL Saline/PBS/ddH2O，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
剂量转换
对于不同动物的给药剂量换算，您也可以参考 更多
