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中文名称: ETP-46464
英文名称: ETP-46464
CAS No: 1345675-02-6
分子式: C30H22N4O2
分子量: 470.52
安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)
E10383 ETP-46464 ≥98% (psaitong)
包装规格：
5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：
溶于DMSO（5 mg/mL 超声）
产品描述：

基本信息

产品编号：

E10383

产品名称：

ETP-46464

CAS:

1345675-02-6

 

储存条件

粉末

-20℃

四年

 

 

分子式：

C30H22N4O2

溶于液体

-80℃

6个月

分子量：

470.52

-20℃

1个月

化学名： 

4-[4-(1-Isocyano-1-methyl-ethyl)-phenyl]-6-quinolin-3-yl-1,4-dihydro-2-oxa-4,9-diaza-phenanthren-3-one;ATRi

Solubility (25°C)：

 

体外:

 

DMSO

14mg/mL (29.75mM)

Ethanol

Insoluble

Water

Insoluble

体内(现配现用):

1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline

Solubility:≥0.5mg/mL(1.06mM);Clear solution

此⽅案可获得 ≥ 0.5 mg/mL (1.06 mM，饱和度未知) 的澄清溶液。 以 1 mL ⼯作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加⼊ 50 μL Tween-80，混合均匀；然后继续加⼊ 450 μL ⽣理盐⽔定容⾄ 1 mL。

＜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

2.1253mL

10.6265mL

21.2531mL

5mM

0.4251mL

2.1253mL

4.2506mL

10mM

0.2125mL

1.0627mL

2.1253mL

 

生物活性

产品描述

一种有效的mTOR和ATR抑制剂，IC50分别为0.6和14nM。

靶点

mTOR;ATM/ATR

体外研究

ETP-46464 (ATRi) also inhibits DNA-PK,PI3Kα and ATM with IC50s of 36nM,170nM and 545nM,respectively.Platinumsensitive and -resistant ovarian, endometrial and cervical cancer cell lines are treated with varying levels of Cisplatin (0-50µM) with or without the ETP-46464 (5.0µM) and/or the KU55933 (10.0µM) for 72h.Single-agent dose response analyses of ETP-46464 and KU55933 in a subset of cell lines reveal a wide LD50 range of 10.0±8.7 and 38.3±7.6µM respectively.Cotreatment doses are chosen based on these studies and previously published evidence of phospho-Chk1 (Ser345) and phospho-ATM (Ser1981) inhibition following ionizing radiation exposure and dose response treatments with ETP-46464 and KU55933.Treatment with ETP-46464 significantly increases the response of Cisplatin in all cell lines tested,resulting in 52-89% enhancement in activity and are synergistic.The combined inhibition of ATR and ATM enhances the response of Cisplatin to a level equivalent to that observed using ETP-46464 alone.These effects are independent of p53 status,and are observed in all gynecologic (GYN) cancer cells tested.Treatment with ETP-46464,but not KU55933,not only sensitizes these GYN cancer cell lines to Cisplatin,but also enhances the response of Carboplatin.

 

推荐实验方法(仅供参考)

激酶实验：

Compounds (e.g.,ETP-46464) and control inhibitors are delivered directly to cell media (100μL per well) with a multi-well pipette at a final concentration of 10μM.Media content is homogenized by carefully vortexing plates at 500 rpm.Prior to 4- hydroxy-tamoxifen (4-OHT) addition,Compounds (e.g.,ETP-46464 ) are incubated at 37ºC for 15 minutes. Next, to induce ATR activity, 4-OHT is added to all wells and incubated for 60 minutes at 37℃.Finally,cells are fixed with paraformaldehyde and processed for IF.Every compound (e.g.,ETP-46464) is analyzed at least in three independent experiments.

 

细胞实验:

 

Cells are trypsinized with 0.25% Trypsin-EDTA and counted with 0.4% Trypan Blue using an automated cell counter and plated in 96-well plates at 5000 cells per well for KLE,HEC1B and HELA and 10,000 cells per well for OVCAR3,A2780,A2780-CP20 and SIHA.After cells attach and reach approximately 60% confluency (24-48h post seeding),media is removed and replaced with fresh media containing Cisplatin (0,0.78,1.56,3.13,6.25,12.5,25 or 50µM) or Carboplatin (0,1.56,3.13,6.25,12.5,25,50 or 100µM) in 0.15% DMSO,5µM ETP-46464,10µM KU55933,or a combination of 5µM ETP-46464 and 10µM KU55933 and incubated for 72h.Final concentrations of ETP-46464 and KU55933 utilized are based on prior evidence indicating inhibition of ATR and ATM signaling,respectively.Single agent dose response analyses of ETP-46464 and KU55933 in a subset of cell lines revealed a wide LD50 range (10.0±8.7 and 38.3±7.6µM,respectively).Similarly,cells are treated with fresh media containing Cisplatin (0,0.78,1.56,3.13,6.25,12.5,25 or 50µM) in 0.08% DMSO and 5 µM VE-821.Cell viability is assessed using the MTS CellTiter 96 Aqueous One Solution Cell Proliferation Assay.After a 2h incubation at 37℃,absorbance is measured at 490nm using a microplate spectrophotometer.Three biological replicates are performed for each cell line where each inhibitor(s)/Cisplatin concentration is assayed in triplicate for each experiment.
保存条件：
-20℃
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
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

  • =
    *
    *
    *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):
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