Sunitinib (SU 11248) 是一种多靶点受体酪氨酸激酶抑制剂，对 VEGFR2 和 PDGFRβ 的 IC50 值分别为 80 nM 和 2 nM。作为一种 ATP 竞争性抑制剂，舒尼替尼有效抑制 Ire1α 的自磷酸化，从而阻止 RNase 激活。

Cabozantinib是一种强效和口服活性的 VEGFR2 和 MET 抑制剂，IC50 值分别为 0.035 和 1.3 nM。它还强效抑制 KIT、RET、AXL、TIE2 和 FLT3，IC50 值分别为 4.6、5.2、7、14.3 和 11.3 nM。Cabozantinib 显示出抗血管生成活性，破坏肿瘤血管结构，并促进肿瘤和内皮细胞凋亡。

Ponatinib (AP24534) 是一种口服活性的多靶点激酶抑制剂，对 Abl 的 IC50 为 0.37 nM，对 PDGFRα 为 1.1 nM，对 VEGFR2 为 1.5 nM，对 FGFR1 为 2.2 nM，对 Src 为 5.4 nM。

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.

PD173074是一种有效的FGFR1抑制剂，IC50为25 nM。它还抑制VEGFR2的活性，IC50为100-200 nM，对FGFR1与PDGFR和c-Src的选择性超过1000倍。

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.

RAF265 is a pan-inhibitor that inhibits C-Raf, B-Raf and B-Raf V600E with IC50 of 3 nM-60 nM. It also shows inhibition on phosphorylation of VEGFR2 with EC50 of 30 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.

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.

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.