产品说明书

MGCD-265 analog

Print
Chemical Structure| 875337-44-3 同义名 : MGCD-265
CAS号 : 875337-44-3
货号 : A209718
分子式 : C26H20FN5O2S2
纯度 : 99%+
分子量 : 517.598
MDL号 : MFCD17779287
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(202.86 mM)，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：
生物活性
靶点

  • VEGFR1

    VEGFR1, IC50:3 nM

  • VEGFR3

    VEGFR3, IC50:4 nM

  • VEGFR2

    VEGFR2, IC50:3 nM

  • Tie-2

    Tie-2, IC50:7 nM
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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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 ... 展开 >> Karmanos Cancer Institute Detroit, Michigan, United States, 48201 United States, Texas University of Texas M.D. Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT00975767 Advanced Malignancies, Non-sma... 展开 >>ll Cell Lung Cancer 收起 << Phase 1 Terminated(The study was termi... 展开 >>nated due to a need for a reformulation of the study drug. Phase 1 completed, no patients enrolled in Phase 2.) 收起 << - United States, Michigan ... 展开 >> 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 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.66mL

1.93mL

0.97mL

19.32mL

3.86mL

1.93mL
参考文献

[1]Claridge S, Raeppel F, et al. Discovery of a novel and potent series of thieno[3,2-b] pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. Bioorg Med Chem Lett. 2008 May 1;18(9):2793-8.