Tie2 kinase inhibitor 1 is a strong and selective inhibitor of Tie2 kinase, exhibiting an IC50 value of 250 nM. It has shown an IC50 of 50 μM against p38 and demonstrates moderate to high efficacy in cellular assays, with a cellular IC50 of 232 nM[1]. It exhibits anti-cancer properties[2].
Tie2 kinase inhibitor 1 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HUVEC
2 μM
15 days
Inhibit Tie2 signaling pathway, reduce proangiogenic features of TDEC IR+
Cell Death Dis. 2019 Oct 28;10(11):816.
TDEC IR+
2 μM
15 days
Inhibit Tie2 signaling pathway, reduce proangiogenic features of TDEC IR+
Cell Death Dis. 2019 Oct 28;10(11):816.
Nalm-6 cells
0-200 μM
72 h
Evaluate the cytotoxicity of Tie2 kinase inhibitor on Nalm-6 cells, results showed inhibitor induced cell death in a dose-dependent manner
Cancer Sci. 2018 Dec;109(12):3805-3815.
human retinal microvascular ECs (HRMVECs)
10 µM
21 days
Inhibition of TIE2 signaling to study its effect on microvascular morphology, resulting in thinner vessels with enhanced CLDN5 expression.
Nat Commun. 2024 Feb 14;15(1):1372.
Human primary NF-PitNET cells
5 μM (IC50)
48 h
9 out of 12 samples responded to Tie2-KI with 20-55% reduction in cell viability.
Evaluated the inhibitory effect of Tie2 kinase inhibitor on GH3 cell proliferation, showing >20% suppression.
EMBO Mol Med. 2022 May 9;14(5):e14364.
Megakaryocytic progenitor (MP) cells
250 nM
3 days
To evaluate the recovery effect of Tie2 inhibitor on rhCOMP-Ang1-induced suppression of GATA-1 expression, results showed that Tie2 inhibitor almost completely recovered GATA-1 expression
Stem Cells. 2023 Jan 30;41(1):93-104.
HUVECs
5 µM
48 h
Inhibit TIE2 signaling pathway, reverse the pro-angiogenic effect of TIE2-high cervical cancer cells on HUVECs
Transl Oncol. 2022 Dec;26:101539.
cultured bone marrow-derived endothelial cells (cBEC)
1 mM
To investigate the effect of Tie2 kinase inhibitor on Ang1-induced Notch signaling pathway, results showed that Tie2 inhibitor completely blocked Ang1-induced expression of Notch ligands Dll4 and Jag1.
Haematologica. 2019 Nov;104(11):2164-2177.
TEM (TIE-2 expressing monocytes)
8 μM
36 h
To evaluate the effect of Tie2 kinase inhibitor on the pro-angiogenic activity of TEM, results showed that the inhibitor significantly reduced the pro-angiogenic activity of TEM.
PLoS Comput Biol. 2015 Mar 13;11(3):e1004050.
Tie2 kinase inhibitor 1 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
MatrigelTM plug assay
Intraperitoneal injection
30 mg/kg
Twice daily for 14 days
Inhibit Tie2 signaling pathway, reduce proangiogenic features of TDEC IR+ in vivo
Cell Death Dis. 2019 Oct 28;10(11):816.
Mice
K14-Cre;c-Ang1 and Col2.3-Cre;c-Ang1 transgenic mice
Intraperitoneal injection
10 mg/kg
Single injection
To evaluate the recovery effect of Tie2 inhibitor on GATA-1 expression and platelet levels in transgenic mice, results showed that Tie2 inhibitor restored GATA-1 expression and platelet levels
Stem Cells. 2023 Jan 30;41(1):93-104.
Lewis rats
Neuromyelitis optica (NMO) model
Intraperitoneal injection
25 mg/kg
Daily for 2 weeks
Inhibiting Tie2 kinase resulted in partial loss of C16 peptide-mediated effects, while suppressing PI3K/Akt signaling reduced C16 peptide-mediated effects. In addition, activation of the αvβ3 integrin axis and Tie2 kinase promoted PI3K/Akt signaling.
Front Pharmacol. 2019 Dec 3;10:1373
Tie2 kinase inhibitor 1 动物研究
Animal study
Administered intraperitoneally at a dosage of 50 mg/kg twice weekly for six weeks, Tie2 kinase inhibitor 1 leads to a statistically significant decrease in tumor size by the 15th day. By the 20th day, it achieves a 61% reduction in tumor volume, and by the end of the 6-week period, the reduction in tumor volume is 45%[1].
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