1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. VEGFR-2-IN-47

VEGFR-2-IN-47 (compound 7g) 是一种有效的 VEGFR-2 抑制剂,IC50 值为 0.072 μM。VEGFR-2-IN-47 可诱导 MCF-7 细胞进入 G2 / M 期细胞周期停滞,促进细胞凋亡,并通过下调 TNF-α 的水平和上调 IL-2 的水平来增强免疫调节。VEGFR-2-IN-47 具有用于乳腺癌和肝癌等癌症研究的潜力。

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VEGFR-2-IN-47 Chemical Structure

VEGFR-2-IN-47 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VEGFR-2-IN-47 (compound 7g) is a potent VEGFR-2 inhibitor with an IC50 value of 0.072 µM. VEGFR-2-IN-47 can induce G2 / M phase cell cycle arrest, promote apoptosis, and boost immunomodulation by downregulating TNF-α expression and upregulating IL-2 levels in MCF-7 cells. VEGFR-2-IN-47 has the potential to be used for the research of cancer such as breast cancer and liver carcinoma [1].

IC50 & Target

VEGFR2

0.072 μM (IC50)

体外研究
(In Vitro)

VEGFR-2-IN-47 (compound 7g) (48 h) 对 MCF-7 和 HepG2 癌细胞展现出高度选择性的抗增殖活性,IC50 值分别为 19.35 和 27.89 μM。VEGFR-2-IN-47 对正常细胞(WI-38)毒性较低,IC50 值为 51.14 μM,显示出良好的安全性[1]
VEGFR-2-IN-47 (19.35 μM; 72 h) 导致 MCF-7 细胞在 G0 / G1 和 S 期减少,在 G2 / M 期积累[1]
VEGFR-2-IN-47 (19.35 μM; 72 h) 可通过下调 MCF-7 细胞中 Bcl-2 的水平和上调 Bax 的水平促进细胞凋亡,以及通过下调 TNF-α 的水平和上调 IL-2 的水平来增强免疫调节[1]

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

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 19.35 μM
Incubation Time: 72 hours
Result: Increased the cell population at the G2 / M phase compared to untreated cells from 16.41 to 24.89 %. Induced a decrease in the cell population at the G0 - G1 phase (from 59.04 to 54.51 %) and S phase (from 24.55 to 20.60 %).

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 19.35 μM
Incubation Time: 72 hours
Result: Showed a significant increase in early and late apoptosis (17.65 and 7.21 %, respectively) compared to untreated cells (0.43 and 1.71 %, respectively).

Real Time qPCR[1]

Cell Line: MCF-7 cells
Concentration: 19.35 μM
Incubation Time: 72 hours
Result: Upregulated the expression of Bax by more than 4.5 times and downregulated Bcl-2 by more than 6 times. Exhibited a strong suppressive effect on the TNF-a (2.5 fold) and stimulatory effect on the IL-2 (3.3 fold) compared to the control cells.
分子量

446.46

Formula

C23H22N6O4

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
VEGFR-2-IN-47
目录号:
HY-163747
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