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Axitinib是一种多靶点酪氨酸激酶抑制剂,对VEGFR1、VEGFR2、VEGFR3和PDGFRβ的IC50值分别为0.1 nM、0.2 nM、0.1-0.3 nM和1.6 nM。
Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Foretinib is less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and with little activity to FGFR1 and EGFR.
Nintedanib(BIBF 1120)是一种强效的三重血管激酶抑制剂,对VEGFR1/2/3、FGFR1/2/3和PDGFRα/β的IC50值分别为34 nM、13 nM、13 nM、69 nM、37 nM、108 nM、59 nM和65 nM。
Regorafenib(BAY 73-4506)是一种口服活性和高效的多靶点受体酪氨酸激酶抑制剂,对VEGFR1/2/3、PDGFRβ、Kit、RET和Raf-1的IC50值分别为13/4.2/46、22、7、1.5和2.5 nM。Regorafenib显示出强大的抗肿瘤和抗血管生成活性。
Pazopanib(GW786034)是一种新型多靶点抑制剂,对VEGFR1、VEGFR2、VEGFR3、PDGFRβ、c-Kit、FGFR1和c-Fms的IC50值分别为10 nM、30 nM、47 nM、84 nM、74 nM、140 nM和146 nM。
Cediranib is a multiple RTKs inhibitor with IC50 values of <0.001μM, 0.005μM, ≤0.003μM, 0.002μM and 0.005μM for VEGFR-2, VEGFR-1, VEGFR-3, c-Kit and PDGFR-β(measured kinase activity), respectively.
Linifanib is a potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively.
Vatalanib 2HCl is inhibitor of VEGFR2 or KDR with IC50 of 37 nM.
Tivozanib is an inhibitor of VEGFR1, VEGFR2 and VEGFR3 with IC50s of 30 nM, 6.5 nM, 15 nM, respectively. It can also inhibit PDGFR and c-Kit.
Lenvatinib(E7080)是一种口服、多靶点的酪氨酸激酶抑制剂,靶向VEGFR1-3、FGFR1-4、PDGFR、KIT和RET,显示出强效的抗肿瘤活性。
Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but > 240-fold against PDGFR-β.
MGCD-265, an ATP-competitive inhibitor, can inhibit c-Met and VEGFR1, 2, 3 with IC50s of 1 nM and 3 nM, 3 nM, 4 nM, respectively. It also exhibits inhibition of Ron and Tie2.
OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively and also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl.
ZM-306416 is an inhibitor of VEGFR (Flk-1 or KDR) and Flt with IC50 of 100 nM and 2 μM. It also shows inhibition activity against Src and Abl with IC50 values of 0.33μM and 1.3μM, respectively.
Sitravatinib is an inhibitor of receptor tyrosine kinase (RTK) involved in driving sarcoma cell growth, is developed for the treatment of cancer.
BAW2881 is an inhibitor of vascular endothelial growth factor (VEGF) with IC50s of 1.0 nM-4.3 nM against VEGFR1, 2, 3 and also inhibits PDGFRβ, c-Kit, and RET.
Dovitinib is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM.
Motesanib diphosphate is ATP-competitive inhibitor of VEGFR1, VEGFR2 and VEGFR3 with IC50 of 2 nM, 3 nM and 6 nM, respectively. It also shows better inhibitory activity against c-Kit, PDGFR, and RET.
AEE788 is an inhibitor of both EGFR and VEGFR, the IC50s for EGFR and ErbB2 is 2 nM, 6 nM respectively.
KRN-633 can inhibit VEGFR1, VEGFR2 and VEGFR3 with IC50 of 170 nM, 160 nM, and 125 nM, respectively.
Tags: VEGFR1 | VEGFR | VEGFR1 相关产品
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