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编 号：F744847
分子式：C19H21N5O3
分子量：367.4
分子式：C19H21N5O3
分子量：367.4
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CAS No: 1412453-70-3
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生物活性：
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.
体内研究：
EVT801 (30 mg/kg; p.o.; twice daily for 7 d) shows inhibitory effect on VEGFR-3-positive tumors in mouse models, such as RT-001-HAM Subcutaneous Patient-derived xenograft (PDx) Tumor Mouse Model, 4T1 Mammary Carcinoma Mouse Model, N-diethylnitrosamine-Induced Hepatocarcinoma Mouse Model, NCI-H1703 Subcutaneous Xenograft Tumor Mouse Model, Rip1-Tag2/transgenic Mouse Models, and CT26 Ectopic Tumor Mouse Model. EVT801 is expressed in blood vessels of kidney cancer primary tumors and metastases, and in tumor cells of endothelial malignancies.
体外研究：
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.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.EVT801 (1 μM) inhibits proliferation and tumor growth of VEGFR-3-positive tumor cells.
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.
体内研究：
EVT801 (30 mg/kg; p.o.; twice daily for 7 d) shows inhibitory effect on VEGFR-3-positive tumors in mouse models, such as RT-001-HAM Subcutaneous Patient-derived xenograft (PDx) Tumor Mouse Model, 4T1 Mammary Carcinoma Mouse Model, N-diethylnitrosamine-Induced Hepatocarcinoma Mouse Model, NCI-H1703 Subcutaneous Xenograft Tumor Mouse Model, Rip1-Tag2/transgenic Mouse Models, and CT26 Ectopic Tumor Mouse Model. EVT801 is expressed in blood vessels of kidney cancer primary tumors and metastases, and in tumor cells of endothelial malignancies.
体外研究：
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.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.EVT801 (1 μM) inhibits proliferation and tumor growth of VEGFR-3-positive tumor cells.
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