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VEGFR/PDGFR 抑制剂/激活剂/调节剂 Vascular Endothelial Growth Factor Receptor/platelet-derived growth factor receptor

目录号 产品名称 产品简介
M1658 Axitinib Axitinib是一种多靶点抑制剂,作用于VEGFR-1, VEGFR-2,VEGFR-3,PDGFR-β和c-KIT时,其IC50分别为0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM和1.7 nM。
M2194 SU5402 SU 5402是VEGFR2和FGFR1的多靶点抑制剂,IC50分别为20和30 nM。
M1838 Masitinib Masitinib (AB1010)是一种新型的Kit和PDGFRα/β抑制剂,IC50分别为200 nM和540 nM/800 nM,但对ABL和c-Fms抑制作用较弱。Phase 2/3。
M1956 Apatinib mesylate Apatinib是一种口服生物有效性的VEGFR2选择性抑制剂,IC50为1 nM 。
M1841 Lenvatinib 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。
M20877 Toceranib phosphate Toceranib phosphate is a multitargeted indolinone receptor tyrosine kinase (RTK) inhibitor with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively.
M20835 Seralutinib (GB002) Seralutinib (PK10571, GB002) is a novel PDGFR kinase inhibitor with IC50s of 8 nM and 10 nM for PDGFRα and PDGFRβ in enzyme assays, respectively.
M20740 SU5204 SU5204 is a tyrosine kinase inhibitor with IC50 of 4 μM and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively.
M20715 CS-2660 (JNJ-38158471) CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as Ret and Kit with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3.
M20700 Vorolanib (X-82) Vorolanib is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities.
M20586 ZD-4190 ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.
M20360 WAY-302159 WAY-302159 is a novel VEGFR-2 inhibitor.
M20358 WAY-340935 WAY-340935 is a VEGFR2 kinase inhibitor.
M20248 WAY-637081 WAY-637081 is a VEGFR2 inhibitor
M20201 WAY-607500 WAY-607500 is a VEGFR inhibitor.
M20170 WAY-357919 WAY-357919 is a inhibitor of vascular endothelial growth factor receptor-2.
M20107 WAY-325185 WAY-325185 altering the lifespan of a eukaryotic organism
M20062 WAY-297629 WAY-297629 is a VEGFR2 inhibitor.
M20044 WAY-271147 WAY-271147 is a VEGFR inhibitor
M20043 WAY-271146 WAY-271146 is a VEGFR inhibitor
M20021 GI-555736 GI-555736 altering the lifespan of a eukaryotic organism
M20019 CL-230482 CL-230482 is a PDGFR inhibitor.
M20016 AY-20590 AY-20590 is a inhibitor of Mcl-1 (for the treatment of cancer and other diseases).
M14922 TG 100801 TG 100801 是TG 100572的前药,通过去酯化产生TG 100572,开可用于黄斑变性的研究。TG 100572 是多靶点激酶抑制剂,抑制受体酪氨酸激酶 (receptor tyrosine kinases) 和Src激酶 (Src kinases); 对VEGFR1,VEGFR2,FGFR1,FGFR2,PDGFRβ,Fgr,Fyn,Hck,Lck,Lyn,Src,Yes 的 IC50 值分别为2,7,2,16,13,5,0.5,6,0.1,0.4,1,0.2。
M14921 Telatinib mesylate Telatinib mesylate (Bay 57-9352 mesylate) 是一种有效的的口服活性的 VEGFR2,VEGFR3,PDGFα 和 c-Kit 抑制剂,IC50 分别为 6 nM,4 nM,15 nM 和 1 nM。









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