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AZD1390 {[allProObj[0].p_purity_real_show]}

货号：A775616

AZD1390 is an ATM inhibitor with IC50 of 0.78 nM in cells.

AZD1390 化学结构 CAS号：2089288-03-7
AZD1390 化学结构
CAS号：2089288-03-7
AZD1390 3D分子结构
CAS号：2089288-03-7
AZD1390 化学结构 CAS号：2089288-03-7
AZD1390 3D分子结构 CAS号：2089288-03-7
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AZD1390 纯度/质量文件 产品仅供科研

货号：A775616 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 ATM ↓ ATR ↓ 其他靶点 纯度
Wortmannin ++

ATM, IC50: 150 nM

 		PI3K,DNA-PK,MLCK 99%+
CP-466722 +

ATM, IC50: 410 nM

 		99%+
Torin 2 ++

ATM, EC50: 28 nM

 		++

ATR, EC50: 35 nM

 		mTOR,DNA-PK 99%+
KU-55933 +++

ATM, IC50: 12.9 nM

 		96%
ETP-46464 +

ATM, IC50: 545 nM

 		+++

ATR, IC50: 14 nM

 		mTOR,DNA-PK 98%
CGK733 ++

ATM, IC50: 200 nM

 		++

ATR, IC50: 200 nM

 		99%+
AZD0156 ✔ 99%+
Dactolisib +++

ATR, IC50: 21 nM

 		98+%
Ceralasertib ++++

ATR, IC50: 1 nM

 		99%+
Berzosertib +++

ATR, IC50: 19 nM

 		99%+
VE-821 +++

ATR, Ki: 13 nM

 		99%+
AZ20 ++++

ATR, IC50: 5 nM

 		mTOR 99%+
Schizandrin B +

ATR, IC50: 7.25 μM

 		P-gp 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

AZD1390 生物活性

描述 The ataxia-telangiectasia mutated (ATM) protein kinase is a master regulator of the DNA damage response (DDR), and it coordinates checkpoint activation, DNA repair, and metabolic changes in eukaryotic cells in response to DNA double-strand breaks and oxidative stress[1]. AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC50 of 0.78 nM in cell[2]. AZD1390 blocks ATM-dependent DDR pathway activity and combines with radiation to induce G2 cell cycle phase accumulation, micronuclei, and apoptosis. AZD1390 radiosensitizes glioma and lung cancer cell lines, with p53 mutant glioma cells generally being more radiosensitized than wild type[2]. In in vivo syngeneic and patient-derived glioma as well as orthotopic lung-brain metastatic models, AZD1390 dosed in combination with daily fractions of ionizing radiation (IR) (whole-brain or stereotactic radiotherapy) significantly induced tumor regressions and increased animal survival compared to IR treatment alone[2].

AZD1390 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03215381 Healthy Volunteer Male Subject... 展开 >>s 收起 << Phase 1 Completed - Sweden ... 展开 >> Research Site Stockholm, Sweden, 171 76 收起 <<
NCT03423628 Recurrent Glioblastoma Multifo... 展开 >>rme Primary Glioblastoma Multiforme Brain Neoplasms, Malignant Leptomeningeal Disease (LMD) 收起 << Phase 1 Recruiting April 5, 2021 United States, Massachusetts ... 展开 >> Research Site Recruiting Boston, Massachusetts, United States, 02215 United States, New York Research Site Recruiting New York, New York, United States, 10065 United States, Pennsylvania Research Site Recruiting Pittsburgh, Pennsylvania, United States, 15232 United States, Virginia Research Site Recruiting Richmond, Virginia, United States, 23294 United Kingdom Research Site Recruiting Cambridge, United Kingdom, CB2 0QQ Research Site Recruiting Glasgow, United Kingdom, G12 0YN Research Site Recruiting Leeds, United Kingdom 收起 <<

AZD1390 参考文献

[1]Paull TT. Mechanisms of ATM Activation. Annu Rev Biochem. 2015;84:711-38. doi: 10.1146/annurev-biochem-060614-034335. Epub 2015 Jan 12. PMID: 25580527.

[2]Durant ST, Zheng L, Wang Y, Chen K, Zhang L, Zhang T, Yang Z, Riches L, Trinidad AG, Fok JHL, Hunt T, Pike KG, Wilson J, Smith A, Colclough N, Reddy VP, Sykes A, Janefeldt A, Johnström P, Varnäs K, Takano A, Ling S, Orme J, Stott J, Roberts C, Barrett I, Jones G, Roudier M, Pierce A, Allen J, Kahn J, Sule A, Karlin J, Cronin A, Chapman M, Valerie K, Illingworth R, Pass M. The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models. Sci Adv. 2018 Jun 20;4(6):eaat1719. doi: 10.1126/sciadv.aat1719. PMID: 29938225; PMCID: PMC6010333.

AZD1390 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.47mL

2.09mL

1.05mL

20.94mL

4.19mL

2.09mL

AZD1390 技术信息

CAS号2089288-03-7
分子式C27H32FN5O2
分子量 477.574
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 4 mg/mL(8.38 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: AZD1390 | 2089288-03-7 | AZD 1390 | AZD-1390 | ATM Inhibitor | Cell Cycle/DNA Damage | PI3K/Akt/mTOR | ATM/ATR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | AZD1390 纯度/质量文件 | AZD1390 亚型比较 | AZD1390 生物活性 | AZD1390 临床数据 | AZD1390 参考文献 | AZD1390 实验方案 | AZD1390 技术信息

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