Compound 401 - CAS:168425-64-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Compound 401
英文名称:	Compound 401
别名:	Compound 401 2-(4-MORPHOLINYL)-4H-PYRIMIDO[2,1-A]ISOQUINOLIN-4-ONE
CAS No:	168425-64-7	分子式:	C₁₆H₁₅N₃O₂	分子量:	281.31
CAS No:	168425-64-7
分子式:	C₁₆H₁₅N₃O₂
分子量:	281.31

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C10918 Compound 401 ≥98% (psaitong)

相关产品

包装规格：

5mg 25mg 50mg 100mg in glass bottle

溶解性：

溶于DMSO（6 mg/mL 超声，加热）

产品描述：

基本信息

产品编号：	C10918
产品名称：	Compound 401
CAS:	168425-64-7	储存条件	粉末	-20℃	四年

分子式：	C16H15N3O2		溶于液体	-80℃	两年
分子量	281.31			-20℃	一个月
化学名：	4H-PyriMido[2,1-a]isoquinolin-4-one, 2-(4-Morpholinyl)-
Solubility (25°C)：
体外:	DMSO	7mg/mL (24.88mM)
	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	3.5548mL	17.7740mL	35.5480mL
5mM	0.7110mL	3.5548mL	7.1096mL
10mM	0.3555mL	1.7774mL	3.5548mL

生物活性

产品描述

一种合成的 DNA-PK (IC50=0.28μM) 抑制剂，在体外也靶向作用于 mTOR，但对 PI3K 没有抑制效果。

靶点

DNA-PK
(Cell-free assay)

0.28μM

mTOR
(Cell-free assay)

5.3μM

体外研究

Compound 401 is a potent inhibitor of DNA-PK (IC50=0.28μM). Compound 401 is reported to be a poor inhibitor of PI3K, ATM, and ATR in vitro, but it is active against mTOR. Compound 401 shows activity against mTOR (IC50=5.3μM) but not p110α/p85 α PI3K (IC50>100μM). Treatment of cells with Compound 401 blocks the phosphorylation of sites modified by mTOR-Raptor and mTOR-Rictor complexes (ribosomal protein S6 kinase 1 Thr³⁸⁹ and Akt Ser⁴⁷³, respectively). By contrast, there is no direct inhibition of Akt Thr³⁰⁸ phosphorylation, which is dependent on PI3K. Similar effects are also observed in cells that lack DNA-PK. Compound 401 inhibits immunoprecipitated epitope-tagged mTOR or endogenous mTOR in Raptor immunoprecipitates. In both cases, inhibition of 67% or 78% is obtained at 5μM or 10μM Compound 401, respectively. By contrast, dose response curves show that the p110α/p85α or p110β/p85α PI3K complexes are poorly inhibited by Compound 401 at these concentrations. The proliferation of TSC1-/- fibroblasts is inhibited in the presence of Compound 401, but TSC1 +/+ cells are resistant

推荐实验方法(仅供参考)

Kinase Assay

FreeStyle 293-F cells are transfected with cDNA for AU1-mTOR using 293fectin. Two days later, the cells are lysed and mTOR immunoprecipitates are prepared using AU1 antibody. Alternatively, the mTORC1 complex is immunoprecipitated from untransfected cells using Raptor antibody. Kinase activity in the immunoprecipitates is assayed in the presence of vehicle (DMSO) or Compound 401 (1, 5 and 10μM) using bacterially expressed glutathione S-transferase (GST)-4E-BP1 as a substrate. Kinase reactions are stopped by boiling in SDS sample buffer and the samples are subjected to SDS-PAGE. Phosphorylated 4E-BP1 is detected by autoradiography. Radioactivity in the bands is quantified by scintillation counting

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 )

* = *

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初始浓度:
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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

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