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CAS No.: 2089288-03-7

AZD1390 Catalog No. CSN23317

Synonyms: AZD1390

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

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技术信息

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].
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... more >>s Collapse <<	Phase 1	Completed	-	Sweden ... more >> Research Site Stockholm, Sweden, 171 76 Collapse <<
NCT03423628	Recurrent Glioblastoma Multifo... more >>rme Primary Glioblastoma Multiforme Brain Neoplasms, Malignant Leptomeningeal Disease (LMD) Collapse <<	Phase 1	Recruiting	April 5, 2021	United States, Massachusetts ... more >> 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 Collapse <<

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0939 mL
- 10.4696 mL
- 20.9392 mL
- 5 mM
- 0.4188 mL
- 2.0939 mL
- 4.1878 mL
- 10 mM
- 0.2094 mL
- 1.0470 mL
- 2.0939 mL

技术信息

CAS号

2089288-03-7

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H32FN5O2

运输

蓝冰

分子量

477.57

别名

AZD1390

溶解度

DMSO	insoluble
Water	insoluble
Ethanol	insoluble

动物实验配方

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