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VEGFR-3-IN-1

CAS No. : 2756668-73-0

MCE 国际站：VEGFR-3-IN-1

产品活性：VEGFR-3-IN-1 是一种有效的高选择性 VEGFR3 抑制剂，其 IC₅₀ 为 110.4 nM。VEGFR-3-IN-1 通过使 VEGFR3 信号通路失活，显著抑制 VEGF-C 诱导人真皮淋巴管内皮细胞 (HDLEC)、MDA-MB-231 和 MDA-MB-436 细胞的增殖和迁移，并且能有效抑制乳腺癌的生长。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：VEGFR

In Vitro: VEGFR-3-IN-1 (compound 38k) exhibits a significantly higher antiproliferative activity on MDA-MB-231 and MDA-MB-436 cells than 10 (IC₅₀ > 50 μM), with IC₅₀ values of 2.22 and 3.50 μM, respectively.
VEGFR-3-IN-1 markedly suppresses the phosphorylation of VEGFR3 and its downstream proteins in a dose-dependent manner.

In Vivo: VEGFR-3-IN-1 (50, 25 mg/kg; p.o.) reduces the tumor volume, and displays the strongest inhibitory activity in mice, with a growth inhibition rate of 61.9%.
VEGFR-3-IN-1 (10 mg/kg; p.o.) treatment shows the C_max, AUC_0-t , AUC_0-∞ and t_1/2 values of 420 ng/mL, 9219 ng h/mL, 12304 ng h/mL and 16 hours, respectively.

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