| Bioactivity | 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]. |
| Invitro | EVT801 (10 nM-1 μM) 剂量依赖性地抑制 HEK293 细胞中 VEGFR-1/2/3 自磷酸化，IC50 分别为39 nM (VEGFR-3)， 2130 nM (VEGFR-1)， 260 nM (VEGFR-2)[1]。EVT801 (1 nM-1 μM) 阻止 VEGFR-3 阳性细胞的增殖，例如人淋巴微血管内皮细胞 (hLMVEC)。EVT801 剂量依赖地抑制 hLMVEC 的增殖诱导，对不同 VEGF 诱导的 IC50 分别为 15 nM (VEGF-C)，8 nM (VEGF-D)，155 nM (VEGF-A)[1]。EVT801 (1 μM) 抑制 VEGFR-3 阳性肿瘤细胞的增殖和肿瘤生长[1]。 Cell Proliferation Assay[1] Cell Line: |
| In Vivo | EVT801 (30 mg/kg; 口服给药; 每天 2 次, 共 7 天) 对小鼠模型中的 VEGFR-3 阳性肿瘤具有抑制作用，如在 RT-001-HAM 皮下患者来源的异种移植 (PDx) 肿瘤小鼠模型、4T1 乳腺癌小鼠模型、N-二乙基亚硝胺诱导肝癌小鼠模型、NCI-H1703 皮下异种移植肿瘤小鼠模型、Rip1-Tag2/转基因小鼠模型和 CT26 异位肿瘤小鼠模型等。EVT801 在肾癌原发肿瘤及转移灶血管中表达，在内皮恶性肿瘤细胞中表达[1]。 |
| Name | EVT801 |
| CAS | 1412453-70-3 |
| Formula | C19H21N5O3 |
| Molar Mass | 367.40 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |