|N-(3-((2-((4-(4-乙酰哌嗪-1-基)-2-甲氧基苯基)氨基)-5-(三氟甲基)嘧啶-4-基)氨基)苯基)丙烯酰胺|CsnPharm

CAS No.: 1374640-70-6

N-(3-((2-((4-(4-Acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide Catalog No. CSN13912

Synonyms: CO-1686;AVL-301;CNX-419

CO-1686 functions as an irreversible and mutant-selective inhibitor of EGFRL858R/T790M and EGFRWT with Ki of 21.5 nM and 303.3 nM respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EGFR (T790M, L858R)

Ki:21.5nM EGFR

Ki:303.3nM
描述CO-1686 is an irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT in cell-free assays, respectively.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
A431	~5 μM	Kinase assay	-	inhibits pEGFR with IC50 of >4331 nM	24065731
A431	~5 μM	Growth inhibitory assay	-	GI50=547 nM	24065731
Ba/F3 (ASV)	~10 μM	Growth inhibitory assay	-	IC50=5290 nM	26515464

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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
NCT03257124	Non-Small Cell Lung Cancer Wit... more >>h EGFR T790M Mutation With Brain and/or Leptomeningeal Metastasis Failed Tyrosine Kinase Inhibitors Collapse <<	Phase 2	Recruiting	December 31, 2019	Korea, Republic of ... more >> Department of Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine Recruiting Seoul, Korea, Republic of, 135-710 Contact: Myung-Ju Ahn, M.D. +82-2-3410-3438 silk.ahn@samsung.com Collapse <<
NCT02186301	Non-Small Cell Lung Cancer	Phase 2 Phase 3	Terminated(Sponsor discontinue... more >>d development of CO-1686 for NSCLC) Collapse <<	-	-
NCT02705339	Carcinoma, Non-Small-Cell Lung... more >> Non-Small Cell Lung Cancer Nonsmall Cell Lung Cancer Collapse <<	Phase 2	Withdrawn(Clovis Oncology disc... more >>ontinued rociletinib.) Collapse <<	April 2020	-

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参考文献

[1] Sequist LV, et al. Rociletinib in EGFR-mutated non-small-cell lung cancer. N Engl J Med. 2015 Apr 30;372(18):1700-9.
[2] Walter AO, Sjin RT, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Dec;3(12):1404-15.

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
- 1.8000 mL
- 9.0001 mL
- 18.0001 mL
- 5 mM
- 0.3600 mL
- 1.8000 mL
- 3.6000 mL
- 10 mM
- 0.1800 mL
- 0.9000 mL
- 1.8000 mL

技术信息

CAS号

1374640-70-6

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

C27H28F3N7O3

运输

蓝冰

分子量

555.55

别名

CO-1686;AVL-301;CNX-419

溶解度

DMSO	210.0 mg/mL (378.0 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+30% PEG300+water	4 mg/mL	clear
PO	0.5% CMC-Na	30 mg/mL	suspension

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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

NCT03257124	Non-Small Cell Lung Cancer Wit... more >>h EGFR T790M Mutation With Brain and/or Leptomeningeal Metastasis Failed Tyrosine Kinase Inhibitors Collapse <<	Phase 2	Recruiting	December 31, 2019	Korea, Republic of ... more >> Department of Medicine, Samsung Medical Center, Sungkyunkwan University School of Medicine Recruiting Seoul, Korea, Republic of, 135-710 Contact: Myung-Ju Ahn, M.D. +82-2-3410-3438 silk.ahn@samsung.com Collapse <<
NCT02186301	Non-Small Cell Lung Cancer	Phase 2 Phase 3	Terminated(Sponsor discontinue... more >>d development of CO-1686 for NSCLC) Collapse <<	-	-
NCT02705339	Carcinoma, Non-Small-Cell Lung... more >> Non-Small Cell Lung Cancer Nonsmall Cell Lung Cancer Collapse <<	Phase 2	Withdrawn(Clovis Oncology disc... more >>ontinued rociletinib.) Collapse <<	April 2020	-
NCT02580708	Non-small Cell Lung Cancer	Phase 1 Phase 2	Terminated(Discontinued develo... more >>pment of rociletinib in NSCLC. Stopped enrollment of new patients into all studies involving rociletinib.) Collapse <<	-	United States, Missouri ... more >> Washington University School of Medicine Saint Louis, Missouri, United States, 63110 United States, North Carolina Levine Cancer Institute Charlotte, North Carolina, United States, 28204 United States, Tennessee Tennessee Oncology, PLLC - The Sarah Cannon Research Institute Nashville, Tennessee, United States, 37203 United States, Virginia Virginia Cancer Specialists Fairfax, Virginia, United States, 22031 Collapse <<
NCT01526928	Locally Advanced or Metastatic... more >> Non Small Cell Lung Cancer Collapse <<	Phase 1 Phase 2	Active, not recruiting	August 31, 2019	-
NCT02630186	Non-small Cell Lung Cancer	Phase 1 Phase 2	Completed	-	United States, California ... more >> University of California at Los Angeles Santa Monica, California, United States, 90404 Collapse <<
NCT02147990	Non-small Cell Lung Cancer	Phase 2	Active, not recruiting	August 31, 2019	-
NCT02547675	-	-	-	-	United States, Arizona ... more >> Mayo Clinic Arizona Scottsdale, Arizona, United States, 85024 United States, California Compassionate Care Research Group, Inc. Fountain Valley, California, United States, 92866 Pacific Cancer Care Monterey, California, United States, 93940 Sutter Cancer Institute Sacramento, California, United States, 95816 UCSF Helen Diller Family Comprehensive Cancer Center San Francisco, California, United States, 94115 United States, Florida Halifax Health - Center for Oncology Daytona Beach, Florida, United States, 32114 UF Health Center Orlando Orlando, Florida, United States, 32806 United States, Massachusetts Beth Israel Deaconess Medical Center Boston, Massachusetts, United States, 02215 United States, Michigan Henry Ford Hospital Detroit, Michigan, United States, 48202 United States, Montana Billings Clinic Billings, Montana, United States, 59101 United States, Oklahoma Tulsa Cancer Institute Tulsa, Oklahoma, United States, 74146 Collapse <<
NCT02322281	Non-small Cell Lung Cancer	Phase 3	Terminated(Sponsor discontinue... more >>d development of CO-1686 for NSCLC) Collapse <<	-	-

靶点	Description	IC50
EGFR (T790M, L858R)		Ki:21.5nM
EGFR		Ki:303.3nM

N-(3-((2-((4-(4-Acetylpiperazin-1-yl)-2-methoxyphenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)phenyl)acrylamide Catalog No. CSN13912

靶点选择性

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