罗米鲁曲 - CAS:192441-08-0 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	罗米鲁曲
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

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L10388 罗米鲁曲 ≥98% (psaitong)

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包装规格：

50mg in glass bottle

溶解性：

溶于DMSO（≥56mg/mL）

产品描述：

基本信息

产品编号：L10388
产品名称：Lomeguatrib
CAS:	192441-08-0	储存条件	粉末	-20℃	四年

分子式：	C10H8BrN5Os		溶于液体	-80℃	六个月
分子量：	326.17			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	65mg/mL (199.28mM)
		Ethanol	Insoluble
		Water	Insoluble
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
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。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	3.0659mL	15.3294mL	30.6589mL
5mM	0.6132mL	3.0659mL	6.1318mL
10mM	0.3066mL	1.5329mL	3.0659mL
50mM	0.0613mL	0.3066mL	0.6132mL

生物活性

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。
靶点/IC50	O6-alkylguanine-DNA-alkyltransferas
靶点/IC50	5nM
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).
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)

激酶实验：

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.

细胞实验:

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.

动物实验:

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.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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参考文献 & 客户发表文献

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

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

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 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果