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KRN-633

CAS No. : 286370-15-8

MCE 国际站：KRN-633

产品活性：KRN-633 是 VEGFR 的有效抑制剂，对VEGFR1，VEGFR2 和 VEGFR3的IC₅₀ 值分别为170，160和125 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：VEGFR

In Vitro: KRN-633 inhibits tyrosine phosphorylation of VEGFR-1, VEGFR2, c-Kit, and PDGFR-β (IC₅₀=11.7, 1.16, 8.01, 130 nM) in human umbilical vein endothelial cells. KRN-633 also inhibits the VEGF-driven proliferation of HUVECs (IC₅₀=14.9 nM). KRN-633 suppresses capillary tube formation of endothelial cells.

In Vivo: KRN-633 inhibits tumor growth in several tumor xenograft models with diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats. KRN-633 also causes the regression of some well-established tumors and those that have regrown after the cessation of treatment. KRN-633 is well tolerated and has no significant effects on body weight or the general health of the animals. Histologic analysis of tumor xenografts treated with KRN-633 reveals a reduction in the number of endothelial cells in non-necrotic areas and a decrease in vascular permeability.

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