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

VS 8 (Compound VS 8) 是一种有效的口服 VEGFR-2 抑制剂，具有显著的抗血管生成 (anti-angiogenic) 作用。 VS 8 诱导癌细胞凋亡 (apoptosis) 和迁移。 VS 8 对 CSCs (癌症干细胞)有活性。

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VS 8 Chemical Structure

VS 8 Chemical Structure

CAS No. : 2471865-38-8

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VS 8 相关抗体

Top Publications Citing Use of Products

查看 VEGFR 亚型特异性产品:

查看所有亚型
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

细胞效力
(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]
体外研究
(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.

VS 8 相关抗体:

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.
体内研究
(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.
分子量

479.45

Formula

C26H20F3N3O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

VS 8 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

Keywords:

VS 82471865-38-8VS8VS-8VEGFRApoptosisReactive Oxygen SpeciesVascular endothelial growth factor receptorMCF-7MDA-MB-231Hep G2HUVECsCancer stem cellsCD44CD133EMTTGF-βInhibitorinhibitorinhibit

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