tie2 kinase inhibitor 1

Tie2 kinase inhibitor 1 (Tie2 kinase inhibitor) 是Tie2激酶选择性抑制剂9IC50:250 nM)，具有抗癌作用。

AMG-Tie2-1 是一种高效的内膜内皮细胞激酶 2 (Tie2) 和 VEGFR2 抑制剂，具有抗癌抗肿瘤活性，可影响心血管生成，可用于研究心血管疾病和癌症。

Tie2 Inhibitor 7 blocks Tie2 kinase activity with a Ki value of 1.3 μM.. It has been shown to inhibit angiopoietin 1-induced Tie2 autophosphorylation and downstream signaling with an IC50 value of 0.3 μM. This compound can prevent endothelial cell tube formation and aberrant vessel growth in a rat model of Matrigel-induced choroidal neovascularization.

N-Desmethyl Regorafenib N-oxide, an active metabolite of the multi-kinase inhibitor regorafenib, originates through the action of the cytochrome P450 (CYP) isoform CYP3A4. This compound demonstrates efficacy in vitro by inhibiting key enzymes such as VEGFR2, Tie2, c-Kit, and B-RAF, and it exhibits tumor growth inhibition in HT-29 and MDA-MB-231 mouse xenograft models at a dosage of 1 mg/kg.

CEP-11981 (tosylate) (ESK981 (tosylate), BOL 303213X (tosylate)) 为一种口服活性的酪氨酸激酶抑制剂 (TKI)，能靶向 TIE2，VEGFR1-3 和 FGFR1，展现出潜在的抗肿瘤及抗血管生成效果。