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- CAS号：
2089288-03-7
- 规格：
1mLx10mM(inDMSO)/1mg/2mg/5mg/10mg/25mg/50mg/100mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥1024.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥542.0 |
| 规格： | 2mg | 产品价格： | ￥782.0 |
| 规格： | 5mg | 产品价格： | ￥984.0 |
| 规格： | 10mg | 产品价格： | ￥1536.0 |
| 规格： | 25mg | 产品价格： | ￥2608.0 |
| 规格： | 50mg | 产品价格： | ￥3576.0 |
| 规格： | 100mg | 产品价格： | ￥5024.0 |
Product Introduction
Bioactivity
| 名称 | azd1390 |
| 描述 | AZD1390 is an exceptionally potent inhibitor of ATM in cells (IC50: 0.78 nM) with >10,000-fold selectivity over closely related members of the PIKK family of enzymes. |
| 细胞实验 | Cells were seeded in six-well plates to a density of 50 to 60% and incubated at 37°C for 24 hours. Cells were pretreated with AZD1390, the ATR inhibitor AZD6738, the Wee1 inhibitor AZD1775, the poly(adenosine diphosphate-ribose) polymerase (PARP) inhibitor olaparib, or the DNA-PK inhibitor KU-0060648 at indicated concentrations for 1 hour and subsequently irradiated at 2 Gy using the Faxitron CellRad (130-kV, 5-mA, 0.5-mm Al). In washout experiments, the cell culture medium was immediately replaced and cells were incubated with or without the compound for 1, 6, and 24 hours. In all other experiments, proteins were collected at indicated time points following irradiation. Proteins were harvested by scraping the cells in radioimmunoprecipitation assay (RIPA) lysis buffer supplemented with protease and phosphatase inhibitors. Protein content was quantified using the BCA Protein Assay Kit according to manufacturing conditions. Proteins were separated by SDS–polyacrylamide gel electrophoresis on 4 to 12% bis-tris or 3 to 8% Tris-acetate gels and transferred onto nitrocellulose membranes using the iBlot Dry Blotting System. Membranes were briefly washed with water and Tris-buffered saline (TBS) with 0.05% Tween 20 (TBST) once and incubated in blocking solution, followed by primary antibodies diluted in TBST with 5% (w/v) nonfat dry milk or 3% bovine serum albumin (BSA) overnight at 4°C with shaking. Membranes were then washed three times and incubated for 1.5 hours with horseradish peroxidase (HRP)–conjugated antibodies and/or LI-COR fluorescent antibodies CW700-800 in TBST with 5% (w/v) nonfat dry milk. Membranes were washed five times with TBST, and proteins were visualized with the Fuji or Syngene G:BOX Imaging System or Film Developer after enhanced chemiluminescence substrate addition. |
| 动物实验 | Bioluminescence signaling of implanted 3 × 10^5 NCI-H2228-Luc cells was measured using an IVIS Xenogen imaging machine to monitor tumor growth. When the signal reached the range of 10^7 to 10^8, the mice were randomized into different treatment groups and treated orally with either vehicle or AZD1390 QD or BID + IR at 2.5 Gy daily for four consecutive days. AZD1390 or vehicle was dosed at 1 hour before IR on each dosing day. The bioluminescence signals and body weight of the mice were measured once weekly, and the raw data were recorded according to their study number and measurement date in the in vivo database. TGI from the start of treatment was assessed by comparison of the mean change in bioluminescence intensity for the control and treated groups and presented as % of TGI. The calculation of inhibition and regression was based on the geometric mean of relative tumor volume (RTV) in each group. "CG" means the geometric mean of RTV of the control group, whereas "TG" means the geometric mean of RTV of the treated group. On specific day, for each treated group, the inhibition value was calculated using the following formula: Inhibition% = (CG ? TG) * 100/(CG ? 1). CG should use the corresponding control group of the treated group during calculation. If inhibition was >100%, then regression was calculated using the following formula: Regression = 1 – TG. Statistical significance was evaluated using a one-tailed t-test. Survival benefit was measured by Kaplan-Meier plots at the end of the study. |
| 体外活性 | AZD1390对ATM自磷酸化的抑制在治疗后4小时发生，3 nM在LN18 GBM细胞中产生了强烈的ATM抑制效果。在相同条件下测试的其他DDR抑制剂，即便是在相关IC50浓度下，也未对pATM水平产生影响。在使用AZD1390及2 Gy辐射处理24小时后，观察到G2阶段累积量呈剂量依赖性增加，这表明细胞没有在S期停滞，而是在G2阶段累积或在有丝分裂过程中遇到问题。 |
| 体内活性 | 在体内同源和患者来源的胶质瘤模型以及原位肺脑转移模型中，AZD1390与每日分割的IR（全脑或立体定向放射治疗）联合使用，显著促进了肿瘤退缩并提高了动物存活率。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 4.84 mg/mL (10.13 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 0.48 mg/mL (1.01 mM), Solution. 10% DMSO+90% Saline : 0.58 mg/mL (1.21 mM), Solution. |
| 关键字 | Inhibitor | inhibit | azd-1390 | azd1390 | AZD 1390 | ATR | ATM/ATR | ATM and RAD3 related | ATM | Ataxia telangiectasia mutated |
| 相关产品 | Schisandrin B | AZD-7648 | ART0380 | VE-821 | Elimusertib | CP-466722 | Tuvusertib | GJ103 sodium salt | GJ071 oxalate | NU6027 | Camonsertib | (Z)-Mirin |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Anti-Aging Compound Library | Highly Selective Inhibitor Library | Anti-Obesity Compound Library | Immunology/Inflammation Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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相关实验
网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 azd1390【2089288-03-7】
￥542 - 5024
