VS 8

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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

CAS No. : 2471865-38-8

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

VEGFR-2

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	1166 nM Compound: VS8	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by trypan blue assay assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by trypan blue assay assay	[PMID: 33002846]
HepG2	IC₅₀	2201 nM Compound: VS8	Antiproliferative activity against human HepG2 cells harboring CD133+ assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human HepG2 cells harboring CD133+ assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33002846]
HepG2	IC₅₀	257.8 nM Compound: VS8	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33002846]
HepG2	IC₅₀	3290 nM Compound: VS8	Antiproliferative activity against human HepG2 cells harboring CD44+ assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human HepG2 cells harboring CD44+ assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33002846]
HUVEC	IC₅₀	9643 nM Compound: VS8	Antiproliferative activity against human HUVEC assessed as reduction in cell viability incubated for 24 hrs by MTT assay Antiproliferative activity against human HUVEC assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33002846]
MCF7	IC₅₀	953.3 nM Compound: VS8	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33002846]
MDA-MB-231	IC₅₀	1413 nM Compound: VS8	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 33002846]
MDA-MB-231	IC₅₀	3577 nM Compound: VS8	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by trypan blue assay assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability by trypan blue assay assay	[PMID: 33002846]

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].

MedChemExpress (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].

MedChemExpress (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
C_max	μg/mL	39.7193 ± 0.36
T_max	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
t_1/2	hrs	11.9277 ± 0.324

Data represented as mean ± SD (n = 3); t_1/2, Half-Life; C_max, Maximum Observed Concentration; T_max, Maximum Observed Time; AUC, Area Under Curve; AUMC Area Under Movement Curve, MRT, Mean Residence Time.

Molecular Weight

479.45

Formula

C₂₆H₂₀F₃N₃O₃

CAS No.

2471865-38-8

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

Handling Instructions (2659 KB)

References

[1]. Siddharth J Modi, et al. Discovery of VEGFR-2 inhibitors exerting significant anticancer activity against CD44+ and CD133+ cancer stem cells (CSCs): Reversal of TGF-β induced epithelial-mesenchymal transition (EMT) in hepatocellular carcinoma. Eur J Med C [Content Brief]

VS 8 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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