|N-((3-氟-4-((2-(1-甲基-1H-咪唑-4-基)噻吩并[3,2-b]吡啶-7-基)氧基)苯基)硫代氨基甲酰基)-2-苯乙酰胺|CsnPharm

CAS No.: 875337-44-3

MGCD-265 analog Catalog No. CSN13151

Synonyms: MGCD-265;MGCD-265 Analog

MGCD-265, an ATP-competitive inhibitor, can inhibit c-Met and VEGFR1, 2, 3 with IC50s of 1 nM and 3 nM, 3 nM, 4 nM, respectively. It also exhibits inhibition of Ron and Tie2.

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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 c-Met

IC50:1nM VEGFR1

IC50:3nM VEGFR2

IC50:3nM VEGFR3

IC50:4nM
描述MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively and also inhibits Ron and Tie2.
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
293T cells	-	Function assay	-	Inhibition of TPR-fused Met phosphorylation expressed in human 293T cells by ELISA, IC50=0.05 μM	19211249
Sf9 cells	-	Function assay	-	Inhibition of GST tagged VEGFR2 expressed in Sf9 cells, IC50=0.01 μM	18434145

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
NCT02954991	Carcinoma, Non-Small-Cell Lung	Phase 2	Recruiting	April 2019	-
NCT00679133	Advanced Malignancies	Phase 1	Completed	-	United States, Michigan ... more >> Karmanos Cancer Institute Detroit, Michigan, United States, 48201 United States, Texas University of Texas M.D. Anderson Cancer Center Houston, Texas, United States, 77030 Collapse <<
NCT00975767	Advanced Malignancies, Non-sma... more >>ll Cell Lung Cancer Collapse <<	Phase 1	Terminated(The study was termi... more >>nated due to a need for a reformulation of the study drug. Phase 1 completed, no patients enrolled in Phase 2.) Collapse <<	-	United States, Michigan ... more >> Barbara Ann Karmanos Cancer Center Detroit, Michigan, United States, 48201 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Pennsylvania University of Pennsylvania Abramson Cancer Center Philadelphia, Pennsylvania, United States, 19104 United States, Texas The University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 South Texas Accelerated Research Therapeutics, LLC San Antonio, Texas, United States, 78229 Collapse <<

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
- 1.9320 mL
- 9.6600 mL
- 19.3200 mL
- 5 mM
- 0.3864 mL
- 1.9320 mL
- 3.8640 mL
- 10 mM
- 0.1932 mL
- 0.9660 mL
- 1.9320 mL

技术信息

CAS号

875337-44-3

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H20FN5O2S2

运输

蓝冰

分子量

517.60

别名

MGCD-265;MGCD-265 Analog

溶解度

DMSO	102.0 mg/mL (197.1 mM)
Water	Insoluble
Ethanol	Insoluble

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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

NCT02954991	Carcinoma, Non-Small-Cell Lung	Phase 2	Recruiting	April 2019	-
NCT00679133	Advanced Malignancies	Phase 1	Completed	-	United States, Michigan ... more >> Karmanos Cancer Institute Detroit, Michigan, United States, 48201 United States, Texas University of Texas M.D. Anderson Cancer Center Houston, Texas, United States, 77030 Collapse <<
NCT00975767	Advanced Malignancies, Non-sma... more >>ll Cell Lung Cancer Collapse <<	Phase 1	Terminated(The study was termi... more >>nated due to a need for a reformulation of the study drug. Phase 1 completed, no patients enrolled in Phase 2.) Collapse <<	-	United States, Michigan ... more >> Barbara Ann Karmanos Cancer Center Detroit, Michigan, United States, 48201 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Pennsylvania University of Pennsylvania Abramson Cancer Center Philadelphia, Pennsylvania, United States, 19104 United States, Texas The University of Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 South Texas Accelerated Research Therapeutics, LLC San Antonio, Texas, United States, 78229 Collapse <<
NCT02117245	-	-	Completed	-	Canada, Quebec ... more >> Algorithme Laval, Quebec, Canada Collapse <<
NCT02544633	Non-Small Cell Lung Cancer	Phase 2	Active, not recruiting	December 2018	-
NCT00697632	Advanced Cancer	Phase 1	Active, not recruiting	December 2018	United States, California ... more >> City of Hope Duarte, California, United States, 91010 UC Irvine Medical Center Orange, California, United States, 92868 UC San Diego San Diego, California, United States, 92093 United States, Illinois University of Chicago Chicago, Illinois, United States, 60637 United States, Massachusetts Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Missouri Washington University, Alvin J. Siteman Cancer Center Saint Louis, Missouri, United States, 63110 United States, New York Columbia University, Herbert Irving Comprehensive Cancer Center New York, New York, United States, 10032 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 United States, Pennsylvania Fox Chase Cancer Center Philadelphia, Pennsylvania, United States, 19111 United States, Texas University of Texas, MD Anderson Cancer Center Houston, Texas, United States, 77030 United States, Utah Huntsman Cancer Institute Salt Lake City, Utah, United States, 84112 United States, Washington Seattle Cancer Care Alliance Seattle, Washington, United States, 98109 Canada, Alberta Cross Cancer Institute Edmonton, Alberta, Canada, T6G 1Z2 Canada, British Columbia British Columbia Cancer Agency, Vancouver Center Vancouver, British Columbia, Canada, V5Z 4E6 Canada, Quebec Jewish General Hospital Montreal, Quebec, Canada, H3T IE2 Korea, Republic of National Cancer Center Gyeonggi-do, Korea, Republic of, 410-769 Seoul National University Hosptial Seoul, Korea, Republic of, 110-744 Samsung Medical Center Seoul, Korea, Republic of, 135-710 Yonsei University Health System, Severance Hospital Seoul, Korea, Republic of Collapse <<
NCT01930006	Advanced Malignancies	Phase 1	Completed	-	United States, Kansas ... more >> Vince & Associates Clinical Research, Inc. Overland Park, Kansas, United States, 66212 Collapse <<

靶点	Description	IC50
c-Met		IC50:1nM
VEGFR1		IC50:3nM
VEGFR2		IC50:3nM
VEGFR3		IC50:4nM

MGCD-265 analog Catalog No. CSN13151

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