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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1412453-70-3
- 分子式: C19H21N5O3
- 分子量:367.40
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
VEGFR アイソフォーム固有の製品をすべて表示
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生物活性
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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 |
化学情報
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CAS 番号 1412453-70-3
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分子量 367.40
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)