EVT801
EVT801 is an orally active and selective inhibitor of VEGFR-3 (IC50=11 nM), which has antitumor effects. EVT801 inhibits not only VEGF-C-induced human endothelial cell proliferation, but also tumor (lymphatic) angiogenesis in tumor mouse models. EVT801 can reduce tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5) and myeloid derived suppressor cells (MDSC) production. EVT801 has synergistic effect with immune checkpoint therapy (ICT), which improves ICT response rate and has better inhibitory effect on cancer mouse models. EVT801 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- CAS No.: 1412453-70-3
- Formule: C19H21N5O3
- Masse moléculaire:367.40
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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VEGFR3 11 nM (IC50) |
VEGFR1 396 nM (IC50) |
VEGFR2 130 nM (IC50) |
ERK 13 nM (IC50) |
EVT801 (10 nM-1 μM) dose-dependently inhibits VEGFR-1/2/3 autophosphorylation in HEK293 cells with IC50s of 39 nM (VEGFR-3), 2130 nM (VEGFR-1), 260 nM (VEGFR-2), respectively[1].
EVT801 (1 nM-1 μM) prevents proliferation of VEGFR-3-positive cells, human lymphatic microvascular endothelial cells (hLMVEC) for example. EVT801 inhibits the induction of hLMVECs proliferation dose-dependently with IC50s of 15 nM (VEGF-C), 8 nM (VEGF-D), 155 nM (VEGF-A), respectively[1].
EVT801 (1 μM) inhibits proliferation and tumor growth of VEGFR-3-positive tumor cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:VEGFR-3-positive cells, human lymphatic microvascular endothelial cells (hLMVEC)
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Concentration:1 nM-1 μM
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Incubation Time:
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Result:Showed a maximum inhibition of 74%, 100%, and 65% against VEGF-C, VEGF-D, VEGF-A induction, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1412453-70-3
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Masse moléculaire 367.40
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Formule C19H21N5O3
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SMILES
O=C1C(C2=NC=CN2)=C(N(C3=NC(C#C[C@@](C)(O)COC)=CC=C31)CC)N
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)