Razuprotafib是一种高效的 VE-PTP (HPTPß) 催化活性抑制剂 (IC₅₀ = 17 pM)，能够激活 TIE2 通路，促进 ANG1 诱导的 TIE2 激活，并刺激下游信号分子如 AKT、eNOS 和 ERK 的磷酸化。Razuprotafib 还对 HPTPη (IC₅₀ = 36 pM) 和 HPTPγ (IC₅₀ = 100 pM) 有抑制作用，具有良好的选择性，并抑制结构相关磷酸酶 PTP1B (IC₅₀ = 780 nM)。

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。

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.

Pexmetinib is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line.

Tie2 kinase inhibitor is an optimized compound of SB-203580, selective to Tie2 with IC50 of 0.25 μM, 200-fold more potent than p38.

CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC50s of 4.7 and 1 nM.

BAY-826 is a selective and potent TIE-2 inhibitor with Kdof 1.6 nM, respectively.

GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2, with a pIC50 of 7.81 for VEGFR2. GW768505A free base has anti-angiogenic activity[1]。