Tubulin/VEGFR-2-IN-2
Tubulin/VEGFR-2-IN-2 is an orally active tubulin and VEGFR-2 inhibitor with IC50s of 3.27 and 0.09 μM, respectively. Tubulin/VEGFR-2-IN-2 exerts the antitumor effects through multifaceted pathways, including enhancing reactive oxygen species (ROS) generation, disrupting mitochondrial membrane potential, inducing apoptosis, and arresting the cell cycle. Tubulin/VEGFR-2-IN-2 demonstrates anti-angiogenic properties by significantly impairing endothelial cell migration, invasion, and tube formation in vitro. Tubulin/VEGFR-2-IN-2 suppresses angiogenesis, tumor growth, and metastasis in vivo. Tubulin/VEGFR-2-IN-2 can be used for non-small lung cancer, breast cancer, gastric cancer and lymphoma.
For research use only. We do not sell to patients.
- CAS No.: 2882998-56-1
- Formula: C20H22N4O3
- Molecular Weight:366.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
VEGFR2 0.09 μM (IC50) |
Tubulin 3.27 nM (IC50) |
In Vitro
Tubulin/VEGFR-2-IN-2 (compound 19d) (48 h) displays superior anti-proliferative effects across a panel of cancer cell lines (IC50 = 0.26, 0.19, 0.04, 0.04, 12.06 and 4.70 μM for A549, MCF-7, MGC-803, U937 cell, HEK 293 T and RAW 264.7 cells respectively) [1].
Tubulin/VEGFR-2-IN-2 (0-20 nM, 24 h) exhibits potent anti-proliferation effects in MGC-803 cells[1].
Tubulin/VEGFR-2-IN-2 (25-100 nM, 48 h) suppresses cell proliferation by interfering with the polymerization process of tubulin in MGC-803 cells[1].
Tubulin/VEGFR-2-IN-2 (25-100 nM, 48 h) reduces the Mitochondrial membrane potential, exhibits apoptosis by activating the caspase family proteins, induces considerable DNA damage and oxidative stress, causes G2/M phase cell cycle arrest and impairs the migratory and invasive ability with a dose-dependent manner in MGC-803 cells[1].
Tubulin/VEGFR-2-IN-2 (20-80 nM, 6-8 h or 48 h) inhibits angiogenesis (including impairs angiogenic structures, destroys the tubular network, decreases nodes, master junctions, segment length, total branching length, meshes, and mean density) by suppressing of the VEGFR-2- driven PI3K/AKT/MAPK pathway in human umbilical vein endothelial cell (HUVEC)[1].
Tubulin/VEGFR-2-IN-2 (20-80 nM, 48 h) inhibits endothelial cell migration and invasion in HUVEC[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MGC-803 cells
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Concentration:25, 50, 100 nM
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Incubation Time:48 h
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Result:Led to a concentration-dependent increase in the proportion of cells in the G2/M phase.
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Cell Line:MGC-803 cells
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Concentration:25, 50, 100 nM
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Incubation Time:48 h
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Result:Transformed from the typical elongated, spindle-like configuration into a rounded form.
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Cell Line:MGC-803 cells
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Concentration:25, 50, 100 nM
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Incubation Time:48 h
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Result:Exhibited concentration-dependent apoptosis.
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Cell Line:MGC-803 cells
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Concentration:25, 50, 100 nM
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Incubation Time:48 h
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Result:Led An upregulation of Cyt-C and the pro-apoptotic protein Bax, accompanied by a downregulation of the anti-apoptotic protein Bcl-2.
Increased in γH2AX expression.
Led a reduction of Cyclin B1 and phosphorylated Cdc2 (p-Cdc2) expression and a marked downregulation of the cell cycle inhibitor P21.
Reduced the phosphorylation of ERK, downregulated the mesenchymal markers Vimentin and N-cadherin, and upregulated the epithelial marker E-cadherin in a dose-dependent manner.
Led to a significant reduction in the expression of both FAK and MMP-9.
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Cell Line:MGC-803 cells
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Concentration:0, 1.25, 2.5, 5, 10 and 20 nM
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Incubation Time:24 h
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Result:Decreased significantly the number and the size of colonies formed.
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Cell Line:MGC-803 cells
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Concentration:25, 50, 100 nM
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Incubation Time:48 h
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Result:Exhibited a significant reduction.
Had an inverse correlation with the invasive capacity of MGC-803 cells.
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Cell Line:HUVEC cells
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Concentration:20, 40 and 80 nM
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Incubation Time:48 h
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Result:Markedly reduced VEGFR-2 expression and attenuated the phosphorylation of PI3K, AKT, and ERK.
Parmacokinetics
In Vivo
Tubulin/VEGFR-2-IN-2 (100-400 nM in 1 mL water, 72 h) effectively inhibits both tumor growth and metastasis in vivo in a dose-dependent manner in fluorescently labeled MGC-803 cells induced-Tg (flk: EGFP) zebrafish larvae[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Tg(flk: EGFP) zebrafish embryos[1]
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Dosage:100 nM, 200 nM, and 400 nM
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Administration:Maintained in 1 mL aquaculture water with different dosage for 18 h
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Result:Produced a dose-responsive decline in both , intersegmental vessels (ISVs) count and vessel length.
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Animal Model:Fluorescently labeled MGC-803 cells (300-500 cells) induced-Tg(flk: EGFP) zebrafish larvae[1]
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Dosage:100 nM, 200 nM, and 400 nM
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Administration:Maintained in 1 mL aquaculture water with different dosage for 18 h
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Result:Suppressed tumor cell migration in a dose-dependent manner.
The tumor mass was significantly decreased at the highest concentration.
Chemical Information
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CAS No. 2882998-56-1
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Molecular Weight 366.41
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Formula C20H22N4O3
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SMILES
NC1=CC(C2=NC(NC3=CC(OC)=C(C(OC)=C3)OC)=NC=C2)=CC=C1C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tubulin/VEGFR-2-IN-2 Related Classifications
HY-180292 Related Classifications
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