2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  3. VEGFR Reactive Oxygen Species (ROS) Apoptosis
  4. VEGFR-2-IN-81

VEGFR-2-IN-81 是一种基于噻唑的异喹啉-1 (2H)-酮衍生物，也是 VEGFR-2 抑制剂，其 IC50 为 1.94 μM。VEGFR-2-IN-81 对结直肠癌细胞表现出显著的选择性细胞毒性 (IC50 = 7.75 μM)。VEGFR-2-IN-81 通过诱导细胞凋亡 (apoptosis)、提升细胞内 ROS 水平和降低线粒体跨膜电位发挥抗结直肠癌作用。VEGFR-2-IN-81 可用于结直肠癌、肺癌、乳腺癌、肝癌的相关研究。

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VEGFR-2-IN-81

VEGFR-2-IN-81 Chemical Structure

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VEGFR-2-IN-81 相关抗体

Top Publications Citing Use of Products

查看 VEGFR 亚型特异性产品:

查看所有亚型
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VEGFR-2-IN-81 is a thiazole-based isoquinolin-1(2H)-one derivative and an VEGFR-2 inhibitor with IC50 of 1.94 μM. VEGFR-2-IN-81 exhibits significant selective cytotoxicity against colorectal cancer cells (IC50 = 7.75 μM). VEGFR-2-IN-81 exerts anti-colorectal cancer effects by inducing apoptosis, elevating intracellular ROS levels and reducing mitochondrial transmembrane potential. VEGFR-2-IN-81 can be used for the research of colorectal cancer, lung cancer, breast cancer, liver cancer[1].

IC50 & Target[1]

VEGFR2

1.94 μM (IC50)

体外研究
(In Vitro)

VEGFR-2-IN-81 (compound 3h) 对多种癌细胞系表现出选择性细胞毒性，在 MCF-7 细胞中的细胞毒性 IC50 值为 25.81 μM，在 HCT-116 细胞中为 7.75 μM，在 A549 细胞中为 14.61 μM，在 HEPG-2 细胞中为 28.27 μM；而对正常 HEK-293 细胞无明显细胞毒性 (IC50 > 35 μM)[1]。
VEGFR-2-IN-81 可抑制纯化的 VEGFR-2 激酶活性，其 IC50 为 1.94 μM[1]。
VEGFR-2-IN-81 (2-15 μM; 24 h) 可呈浓度依赖性诱导人结肠癌细胞 HCT-116 发生凋亡形态学改变及细胞凋亡[1]。
VEGFR-2-IN-81 (2-15 μM; 24 h) 可在体外以浓度依赖的方式升高 HCT-116 人结肠癌细胞内的 ROS 水平[1]。
VEGFR-2-IN-81 (2-15 μM; 24 h) 可在体外以浓度依赖的方式破坏人结肠癌细胞 HCT-116 的线粒体膜电位[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

VEGFR-2-IN-81 相关抗体:

Apoptosis Analysis[1]

Cell Line: HCT-116 human colon cancer cells
Concentration: 2 μM, 7 μM, 15 μM
Incubation Time: 24 h
Result: VEGFR-2-IN-81 (2-15 μM; 24 h) induces apoptotic morphological changes and apoptosis in HCT-116 human colon cancer cells in a concentration-dependent manner.
分子量

470.34

Formula

C21H16BrN3O3S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

VEGFR-2-IN-81 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VEGFR-2-IN-81VEGFRReactive Oxygen Species (ROS)ApoptosisVascular endothelial growth factor receptorHEK-293 cellsHEPG-2 human hepatocellular carcinoma cellsHCT-116 human colon cancer cellsA549 human lung cancer cellsVEGFR-2 inhibitorMCF-7 human breast cancer cellsselective cytotoxicityinduce apoptosiselevate intracellular ROSreduce mitochondrial transmembrane potentialInhibitorinhibitorinhibit

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