|(R)-4-((3-氯-2-氟苯基)氨基)-7-甲氧基喹唑啉-6-基 2,4-二甲基哌嗪-1-羧酸酯|CsnPharm

CAS No.: 1626387-80-1

(R)-4-((3-Chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate Catalog No. CSN16872

Synonyms: AZD3759;zorifertinibum;zorifertinib

AZD3759 is an inhibitor of EGFR (WT), EGFR (L858R) and EGFR (exon 19 deletion) (IC50s values are 0.3 nM, 0.2 nM and 0.2 nM, respectively).

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EGFR (L858R)

IC50:0.2nM EGFR (ex19del)

IC50:0.2nM EGFR

IC50:0.3nM
描述AZD3759 is a potent, oral active, CNS-penetrant EGFR inhibitor with IC50 of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
H3255 cells	-	Proliferation assay	72 h	Antiproliferative against human H3255 cells expressing EGFR L858R mutant after 72 hrs by MTS assay, IC50=0.007 μM	26313252
H838 cells	-	Function assay	-	Inhibition of EGFR phosphorylation in human H838 cells, IC50=0.0645 μM	26313252
PC9 cells	-	Function assay	-	Inhibition of EGFR exon19 deletion mutant phosphorylation in human PC9 cells, IC50=0.0074 μM	26313252

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
NCT03653546	Non-small Cell Lung Cancer ... more >> EGFR Gene Mutation Brain Metastases Collapse <<	Phase 2 Phase 3	Recruiting	October 16, 2021	-
NCT03360929	Non Small Cell Lung Cancer	Phase 1 Phase 2	Recruiting	February 26, 2020	China, Guangdong ... more >> Guangdong General Hospital Recruiting Guangzhou, Guangdong, China, 510080 Contact: Qing Q Zhou 8620-83827812 Collapse <<
NCT02228369	EGFR Mutation Positive Advance... more >>d Non Small Cell Lung Cancer Collapse <<	Phase 1	Active, not recruiting	February 14, 2020	United States, California ... more >> Research Site Los Angeles, California, United States, 90048 Research Site Santa Monica, California, United States, 90404 Australia Research Site Camperdown, Australia, 2050 Research Site Heidelberg, Australia, 3084 Korea, Republic of Research Site Seongnam-si, Korea, Republic of, 463-707 Research Site Seoul, Korea, Republic of, 03080 Research Site Seoul, Korea, Republic of, 03722 Research Site Seoul, Korea, Republic of, 05505 Research Site Seoul, Korea, Republic of, 135-710 Taiwan Research Site Taipei, Taiwan, 100 Collapse <<

参考文献

[1] Yang Z, Guo Q, et al. AZD3759, a BBB-penetrating EGFR inhibitor for the treatment of EGFR mutant NSCLC with CNS metastases. Sci Transl Med. 2016 Dec 7;8(368):368ra172.
[2] Zeng Q, Wang J, et al. Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. J Med Chem. 2015 Oct 22;58(20):8200-15.

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
- 2.1744 mL
- 10.8719 mL
- 21.7438 mL
- 5 mM
- 0.4349 mL
- 2.1744 mL
- 4.3488 mL
- 10 mM
- 0.2174 mL
- 1.0872 mL
- 2.1744 mL

技术信息

CAS号

1626387-80-1

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H23ClFN5O3

运输

蓝冰

分子量

459.90

别名

AZD3759;zorifertinibum;zorifertinib

溶解度

DMSO	92.0 mg/mL (200.0 mM)
Water	Insoluble
Ethanol	44.0 mg/mL (95.7 mM) warming

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03653546	Non-small Cell Lung Cancer ... more >> EGFR Gene Mutation Brain Metastases Collapse <<	Phase 2 Phase 3	Recruiting	October 16, 2021	-
NCT03360929	Non Small Cell Lung Cancer	Phase 1 Phase 2	Recruiting	February 26, 2020	China, Guangdong ... more >> Guangdong General Hospital Recruiting Guangzhou, Guangdong, China, 510080 Contact: Qing Q Zhou 8620-83827812 Collapse <<
NCT02228369	EGFR Mutation Positive Advance... more >>d Non Small Cell Lung Cancer Collapse <<	Phase 1	Active, not recruiting	February 14, 2020	United States, California ... more >> Research Site Los Angeles, California, United States, 90048 Research Site Santa Monica, California, United States, 90404 Australia Research Site Camperdown, Australia, 2050 Research Site Heidelberg, Australia, 3084 Korea, Republic of Research Site Seongnam-si, Korea, Republic of, 463-707 Research Site Seoul, Korea, Republic of, 03080 Research Site Seoul, Korea, Republic of, 03722 Research Site Seoul, Korea, Republic of, 05505 Research Site Seoul, Korea, Republic of, 135-710 Taiwan Research Site Taipei, Taiwan, 100 Collapse <<

靶点	Description	IC50
EGFR (L858R)		IC50:0.2nM
EGFR (ex19del)		IC50:0.2nM
EGFR		IC50:0.3nM

(R)-4-((3-Chloro-2-fluorophenyl)amino)-7-methoxyquinazolin-6-yl 2,4-dimethylpiperazine-1-carboxylate Catalog No. CSN16872

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