VEGFR


VEGF receptors are receptors for vascular endothelial growth factor (VEGF).  There are three main subtypes of VEGFR, numbered 1, 2 and 3. Also, they may be membrane-bound (mbVEGFR) or soluble (sVEGFR), depending on alternative splicing.Vascular endothelial growth factor (VEGF) is an important signaling protein involved in both vasculogenesis (the formation of the circulatory system) and angiogenesis (the growth of blood vessels from pre-existing vasculature). In vitro, VEGF has been shown to stimulate endothelial cell mitogenesis and cell migration. VEGF also enhances microvascular permeability and is sometimes referred to as vascular permeability factor.
  • Lenvatinib EY0870

    Lenvatinib (E7080)是一种多靶点抑制剂,作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效,IC50为4 nM/5.2,对VEGFR1/Flt-1作用效果稍弱,作用于VEGFR2/3比作用于FGFR1, PDGFRα/β选择性高10倍左右。

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  • Semaxanib EY0620

    Semaxanib (SU5416)是一种有效的,选择性的VEGFR(Flk-1/KDR)抑制剂,IC50为1.23 μM,作用于VEGFR比作用于PDGFRβ选择性高20倍,对EGFR, InsR和FGFR没有作用活性。

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  • TSU-68 EY0529

    TSU-68 (SU6668; Orantinib)是多酪氨酸激酶受体抑制剂,对PDGFR自磷酸化抑制性最强,Ki为8 nM,还能相对弱地抑制VEGF-R1和FGF-R1。

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  • Pazopanib EY0458

    Pazopanib, an orally available multi-kinase inhibitor of VEGFR, PDGFR, KIT, FGFR, as well as RAF, shows potent activity against a variety of solid tumors. Pazopanib是多重靶点抑制剂,对VEGFR1, VEGFR2,VEGFR3,PDGFR,FGFR,c-Kit 和 c-Fms的IC50分别为10 nM,30 nM,47 nM,84 nM,74 nM,140 nM和146 nM。

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  • Ponatinib EY0427

    Ponatinib (AP24534)是一种新型有效的作用于Abl, PDGFRα, VEGFR2, FGFR1和Src的多靶点抑制剂, IC50分别为0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM和5.4 nM。

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  • Lenvatinib EY0870

    Lenvatinib (E7080)是一种多靶点抑制剂,作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效,IC50为4 nM/5.2,对VEGFR1/Flt-1作用效果稍弱,作用于VEGFR2/3比作用于FGFR1, PDGFRα/β选择性高10倍左右。

    More
  • Semaxanib EY0620

    Semaxanib (SU5416)是一种有效的,选择性的VEGFR(Flk-1/KDR)抑制剂,IC50为1.23 μM,作用于VEGFR比作用于PDGFRβ选择性高20倍,对EGFR, InsR和FGFR没有作用活性。

    More
  • TSU-68 EY0529

    TSU-68 (SU6668; Orantinib)是多酪氨酸激酶受体抑制剂,对PDGFR自磷酸化抑制性最强,Ki为8 nM,还能相对弱地抑制VEGF-R1和FGF-R1。

    More
  • Pazopanib EY0458

    Pazopanib, an orally available multi-kinase inhibitor of VEGFR, PDGFR, KIT, FGFR, as well as RAF, shows potent activity against a variety of solid tumors. Pazopanib是多重靶点抑制剂,对VEGFR1, VEGFR2,VEGFR3,PDGFR,FGFR,c-Kit 和 c-Fms的IC50分别为10 nM,30 nM,47 nM,84 nM,74 nM,140 nM和146 nM。

    More
  • Ponatinib EY0427

    Ponatinib (AP24534)是一种新型有效的作用于Abl, PDGFRα, VEGFR2, FGFR1和Src的多靶点抑制剂, IC50分别为0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM和5.4 nM。

    More
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