| Identification | Back Directory | [Name]
1,8-Naphthyridin-4(1H)-one, 2-amino-1-ethyl-7-[(3R)-3-hydroxy-4-methoxy-3-methyl-1-butyn-1-yl]-3-(1H-imidazol-2-yl)- | [CAS]
1412453-70-3 | [Synonyms]
EVT801
1,8-Naphthyridin-4(1H)-one, 2-amino-1-ethyl-7-[(3R)-3-hydroxy-4-methoxy-3-methyl-1-butyn-1-yl]-3-(1H-imidazol-2-yl)- | [Molecular Formula]
C19H21N5O3 | [MOL File]
1412453-70-3.mol | [Molecular Weight]
367.4 |
| Hazard Information | Back Directory | [Uses]
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[1]. 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. | [in vivo]
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[1].
| [IC 50]
VEGFR3: 11 nM (IC50); VEGFR1: 396 nM (IC50); VEGFR2: 130 nM (IC50); ERK: 13 nM (IC50) | [References]
[1] Paillasse M R, et al. Targeting Tumor Angiogenesis with the Selective VEGFR-3 Inhibitor EVT801 in Combination with Cancer Immunotherapy[J]. Cancer Research Communications, 2022, 2(11): 1504-1519. |
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