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Referencia número: HY-143491

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VS 8

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).

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No. CAS: 2471865-38-8
Fòrmula: C₂₆H₂₀F₃N₃O₃
Peso molecular:479.45

Almacenamiento:

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

Data Sheet (277 KB)

VS 8 Chemical Structure

No. CAS: 2471865-38-8

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

VEGFR-2

Ver todos los productos específicos de isoformas VEGFR :

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.

Chemical Information

No. CAS 2471865-38-8
Peso molecular 479.45
Fòrmula C₂₆H₂₀F₃N₃O₃
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Calculators

Calculadora de molaridad

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

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Molecular Weight Molecular Weight

Calculadora de dilución

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Concentration _(final) Concentration _(final)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Actividad biológica
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- In Vitro
- In Vivo
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VS 8

Ver todos los productos específicos de isoformas VEGFR

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

VS 8 Related Classifications

HY-143491 Related Classifications