1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. VEGFR2-IN-1

VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC50=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition.

For research use only. We do not sell to patients.

VEGFR2-IN-1 Chemical Structure

VEGFR2-IN-1 Chemical Structure

CAS No. : 2765224-55-1

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Description

VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC50=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition[1].

IC50 & Target

VEGFR2

19.8 nM (IC50)

In Vitro

VEGFR2-IN-1 (compound 17; 0.1, 1, 10, 100 μM; 48 hours) shows an effective and selective agent against MCF-7 (IC50=1.18 μM), MDA-MB-231 (IC50=10.49 μM), MCF-10A (IC50=24.76 μM) cells[1]. VEGFR2-IN-1 (MCF-7 cells; 48 hours) induces cell cycle arrest at the G1 and S-phases[1]. VEGFR2-IN-1 (MCF-7 cells) shows the upregulation of pro-apoptotic genes (p53, Bax, caspases-3, caspases-9) and downregulation of antiapoptotic gene (Bcl-2)[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7, MDA-MB-231, MCF-10A cells
Concentration: 0.1, 1, 10, 100 μM
Incubation Time: 48 hours
Result: Exhibited an effective and selective agent against MCF-7 (IC50=1.18 μM), MDA-MB-231 (IC50=10.49 μM), MCF-10A (IC50=24.76 μM) cells.
In Vivo

VEGFR2-IN-1 (4.2 mg/kg; i.p.; once a day for 7 days) shows anticancer activity with an improvement of hematological, biochemical parameters[1]. Animal Model: Male Swiss albino mice, 21-28 g (Xenograft model)[1].

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

Animal Model: Male Swiss albino mice, 21-28 g (Xenograft model)[1]
Dosage: 4.2 mg/kg
Administration: i.p.; once a days; 7 days
Result: Showed anticancer activity by having a tumor inhibition ratio of 54.2% with an improvement of hematological, biochemical parameters.
Molecular Weight

398.48

Formula

C22H18N6S

CAS No.
SMILES

C=CCSC1=NN=C(N1/N=C/C2=CNC3=CC=CC=C23)C4=CC5=CC=CC=C5N4

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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VEGFR2-IN-1 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:
VEGFR2-IN-1
Cat. No.:
HY-145849
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