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编 号：F753087
分子式：C26H20F3N3O3
分子量：479.45
分子式：C26H20F3N3O3
分子量：479.45
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CAS No: 2471865-38-8
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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).
体内研究：
VS 8 inhibits angiogenesis in the chick chorioallantoic membrane without oral toxicity.Animal Model:Male Wistar rats (180-220 gm)
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) Pharmacokinetic parametersUnit Value
Cmaxμg/mL39.7193 ± 0.36
Tmaxhrs6 ± 0
AUC(0-72)mg/mL*hrs621.3236 ± 1.843
AUC(0-∞)mg/mL*hrs625.2219 ± 1.864
AUMC(0-∞)(mg/mL*hrs2)8929.284 ± 72.85
MRThrs14.2817 ± 0.102
t1/2hrs11.9277 ± 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.
体外研究：
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.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.VS 8 is shown to be a pro-oxidant molecule that enhances the ROS level in Hep G2 cells.VS 8 inhibits wound healing and migration of MCF-7 cancer cells.VS 8 downregulates human vascular endothelial growth factor (hVEGF) and hVEGFR-2 expression in HUVECs.VS 8 (257.80 nM, 48 h) arrests cell cycle at ‘G0/G1’ and ‘S’ phase in CD44+ and CD133+ CSCs, respectively.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.
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).
体内研究：
VS 8 inhibits angiogenesis in the chick chorioallantoic membrane without oral toxicity.Animal Model:Male Wistar rats (180-220 gm)
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) Pharmacokinetic parametersUnit Value
Cmaxμg/mL39.7193 ± 0.36
Tmaxhrs6 ± 0
AUC(0-72)mg/mL*hrs621.3236 ± 1.843
AUC(0-∞)mg/mL*hrs625.2219 ± 1.864
AUMC(0-∞)(mg/mL*hrs2)8929.284 ± 72.85
MRThrs14.2817 ± 0.102
t1/2hrs11.9277 ± 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.
体外研究：
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.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.VS 8 is shown to be a pro-oxidant molecule that enhances the ROS level in Hep G2 cells.VS 8 inhibits wound healing and migration of MCF-7 cancer cells.VS 8 downregulates human vascular endothelial growth factor (hVEGF) and hVEGFR-2 expression in HUVECs.VS 8 (257.80 nM, 48 h) arrests cell cycle at ‘G0/G1’ and ‘S’ phase in CD44+ and CD133+ CSCs, respectively.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.
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