1. Protein Tyrosine Kinase/RTK
    Apoptosis
    Immunology/Inflammation
    NF-κB
    Metabolic Enzyme/Protease
  2. VEGFR
    Apoptosis
    Reactive Oxygen Species
  3. VS 8

VS 8 

Cat. No.: HY-143491
Handling Instructions

VS 8 (Compound VS 8) is a potent, orally active VEGFR-2 inhibitor with significant anti-angiogenic effects. VS 8 induces cancer cell apoptosis and migration. VS 8 is active against CSCs (Cancer stem cells).

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

VS 8 Chemical Structure

VS 8 Chemical Structure

CAS No. : 2471865-38-8

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Description

VS 8 (Compound VS 8) is a potent, orally active VEGFR-2 inhibitor with significant anti-angiogenic effects. VS 8 induces cancer cell apoptosis and migration. VS 8 is active against CSCs (Cancer stem cells)[1].

IC50 & Target

VEGFR-2

 

In Vitro

VS 8 (Compound VS 8) (0.01-100 µM, 24 h) shows potent anti-proliferative activity against MCF-7, MDA-MB-231, Hep G2, and HUVECs cells[1].
VS 8 induces early apoptosis in MDA-MB-231 (1413 nM, 72 h), Hep G2 (257.80 nM, 24 h), and HUVECs (1954 nM, 24 h) cells[1].
VS 8 is shown to be a pro-oxidant molecule that enhances the ROS level in Hep G2 cells[1].
VS 8 inhibits wound healing and migration of MCF-7 cancer cells[1].
VS 8 downregulates human vascular endothelial growth factor (hVEGF) and hVEGFR-2 expression in HUVECs[1].
VS 8 (257.80 nM, 48 h) arrests cell cycle at ‘G0/G1’ and ‘S’ phase in CD44+ and CD133+ CSCs, respectively[1].
VS 8 inhibits TGF-β-induced epithelial-mesenchymal transition (EMT) in hepatocellular carcinoma by the upregulation of E-cadherin and the suppression of vimentin and SNAIL[1].

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

Cell Proliferation Assay[1]

Cell Line: MCF-7, MDA-MB-231, Hep G2, and HUVECs cells
Concentration: 0.01, 0.1, 1, 10, 50, and 100 µM
Incubation Time: 24 h
Result: Showed significantly potent anti-proliferative activity against all the selected cell lines in a dose-dependent manner, with IC50 values of 953.30, 1413, 257.80, and 1954 nM against MCF-7, MDA-MB-231, Hep G2, and HUVECs cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231, Hep G2, and HUVECs cells
Concentration: 1413, 257.80, and 1954 nM for MDA-MB-231, Hep G2, and HUVECs cells, respectively.
Incubation Time: 72 h for MDA-MB-231 cells; 24 h for Hep G2 and HUVECs cells
Result: Resulted in high population of early apoptotic MDA-MB-231 cells (68.34 ± 0.18%). A significant increase in % apoptotic index (~86.66%) was observed in Hep G2 cells. The percentage of early apoptotic cells were found to be ~37.53% in HUVECs cells.

Cell Cycle Analysis[1]

Cell Line: CD44+ and CD133+ CSCs isolated from Hep G2 cells
Concentration: 257.80 nM
Incubation Time: 48 h
Result: Arrested cell cycle at ‘G0/G1’ and ‘S’ phase in CD44+ and CD133+ CSCs, respectively.
In Vivo

VS 8 inhibits angiogenesis in the chick chorioallantoic membrane without oral toxicity[1].

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

Animal Model: Male Wistar rats (180-220 gm)[1]
Dosage: 5 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: Pharmacokinetic parameters for VS 8 in rats after administration of oral dose (5 mg/ kg) [1]
Pharmacokinetic parameters Unit Value
Cmax μg/mL 39.7193 ± 0.36
Tmax hrs 6 ± 0
AUC(0-72) mg/mL*hrs 621.3236 ± 1.843
AUC(0-∞) mg/mL*hrs 625.2219 ± 1.864
AUMC(0-∞) (mg/mL*hrs2) 8929.284 ± 72.85
MRT hrs 14.2817 ± 0.102
t1/2 hrs 11.9277 ± 0.324

Data represented as mean ± SD (n = 3); t1/2, Half-Life; Cmax, Maximum Observed Concentration; Tmax, Maximum Observed Time; AUC, Area Under Curve; AUMC Area Under Movement Curve, MRT, Mean Residence Time.
Molecular Weight

479.45

Formula

C26H20F3N3O3

CAS No.
SMILES

CC(NC1=CC=C(OC2=C3C=CC=C(NC(NC4=CC=CC(C(F)(F)F)=C4)=O)C3=CC=C2)C=C1)=O

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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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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