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

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 .

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VEGFR-2-IN-47 Chemical Structure

VEGFR-2-IN-47 Chemical Structure

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Description

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)

In Vitro

VEGFR-2-IN-47 (compound 7g) (48 h) exhibits highly selective antiproliferative activity against MCF-7 and HepG2 cancer cells with IC50s values of 19.35 and 27.89 µM, respectively. VEGFR-2-IN-47 displays low toxicity to a normal cell line (WI38) with an IC50 value of 51.14 µM, indicating a favorable safety profile[1].
VEGFR-2-IN-47(19.35 μM; 72 h) results in MCF-7 cells reduction in G0 / G1 phase and S phase, accumulation in G2 / M phase[1].
VEGFR-2-IN-47 (19.35 μM; 72 h) can promote apoptosis by downregulating Bcl-2 expression and upregulating Bax levels, and boost immunomodulation by downregulating TNF-α expression and upregulating IL-2 levels in MCF-7 cells[1].

MedChemExpress (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.
Molecular Weight

446.46

Formula

C23H22N6O4

SMILES

CC1=CC=CC(NC(C2=CC=C(C=C2)NC(CN3C(C4=C(N(C3=O)C)N=CN4C)=O)=O)=O)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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VEGFR-2-IN-47 Related Classifications

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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.

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Product Name:
VEGFR-2-IN-47
Cat. No.:
HY-163747
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