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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.
Vandetanib(D6474)是一种有效的口服活性VEGFR2/KDR酪氨酸激酶抑制剂,IC50为40 nM。凡德他尼还抑制VEGFR3/FLT4(IC50=110 nM)和EGFR/HER1(IC50=500 nM)的酪氨酸激酶活性。
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。
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.
ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα.
Telatinib 是一种强效的 VEGFR2/3、c-Kit 和 PDGFRα 抑制剂,IC50 分别为 6 nM/4 nM、1 nM 和 15 nM。
SAR131675 is selective inhibitor of VEGFR3 with IC50 and Ki of 23 nM, 12 nM, 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.
KRN-633 can inhibit VEGFR1, VEGFR2 and VEGFR3 with IC50 of 170 nM, 160 nM, and 125 nM, respectively.
Tags: VEGFR3 | VEGFR | VEGFR3 相关产品
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