tie-2

TIE-2/VEGFR-2 kinase-IN-5 (TIE-2 and VEGFR-2 tyrosine kinase receptor inhibitor) is a potent agent with anti-angiogenic activity, commonly used in biomedical research focused on angiogenesis.

TIE-2/VEGFR-2 kinase-IN-3, a benzimidazole derivative, is a potent inhibitor of tyrosine kinase receptors TIE-2 and VEGFR-2, with IC50 values of 6.9 nM and 3.5 nM, respectively. This compound is useful for angiogenesis research [1].

TIE-2/VEGFR-2 kinase-IN-4, a benzimidazole derivative, is a potent inhibitor of the tyrosine kinase receptors TIE-2 and VEGFR-2, with IC50 values of 5.2 nM and 5.1 nM, respectively. This compound is utilized in angiogenesis research [1].

TIE-2/VEGFR-2 kinase-IN-1 is employed in the synthesis of TIE-2 and/or VEGFR-2 inhibitors for studying diseases associated with inappropriate angiogenesis [1].

Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.

CE-245677 mesylate is a selective Tie2 kinase inhibitor with oral activity and potential antitumor effects, used for pain research.

GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2 (pIC50: 7.81 for VEGFR2) with anti-angiogenic activity.

CE-245677 is a potent, reversible inhibitor of Tie2 and TrkA/B kinases, with cellular IC50 values of 4.7 nM and 1 nM, respectively.

Foretinib (GSK1363089) is a broad-spectrum tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.

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.

Cpd27 (TIE-2/VEGFR-2 kinase-IN-2) is a TIE-2 and VEGFR-2 inhibitor that inhibits RIPK1 and protects RGCs from TNF-stimulated cell death and can be used to study glaucoma.

Tie2 kinase inhibitor 1 (Tie2 kinase inhibitor), an optimized compound of SB-203580, is selective to Tie2 with IC50 of 0.25 μM, which is 200-fold more effective than p38.

2-MT 63 is a novel TIE-2 kinase inhibitor that demonstrates unique and improved kinase selectivity compared to other inhibitors known to interact with TIE-2. 2-MT 63 has a good kinase selectivity profile in enzyme assays with >30-fold selectivity (typically much greater) against the tested kinases. Importantly, the profile includes selectivity against other targets of relevance for angiogenesis (KDR, PDGFR, EPHB4).

Vasculotide, an angiopoietin-1 analog, functions as a Tie-2 activator that induces Tie-2 phosphorylation. This compound exhibits anti-inflammatory properties and enhances vascular permeability. It effectively improves endothelial barrier dysfunction induced by endotoxins and promotes angiogenesis in mouse models of diabetic ulcers. Furthermore, Vasculotide protects mice from vascular leakage and reduces mortality in mouse models of abdominal sepsis. Additionally, it decreases microvascular leakage and improves microcirculation perfusion in rat models of hemorrhagic shock.

Vasculotide TFA is an angiopoietin-1 analog and functions as a Tie-2 activator, inducing Tie-2 phosphorylation. It possesses anti-inflammatory properties and enhances barrier function in endotoxin-induced endothelial dysfunction. Additionally, Vasculotide TFA promotes angiogenesis in murine models of diabetic ulcers and protects mice from vascular leakage, reducing mortality in models of abdominal sepsis. It also reduces microvascular leakage and improves microcirculatory perfusion in rat models of hemorrhagic shock.

SB-633825 can inhibit cancer cell growth and angiogenesis. SB-633825 is an effective and ATP-competitive inhibitor of TIE2, LOK, and BRK (IC50s: 3.5 nM, 66 nM, 150 nM, respectively).

SJ-C1044 is an orally effective pan-RAF inhibitor demonstrating immunomodulatory and antitumor activities. It targets wild-type BRAF, wild-type CRAF, and BRAF(V600E) with IC50 values of 331, 257, and 187 nM, respectively. SJ-C1044 suppresses tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. Additionally, it shows inhibition of VEGFR2, TIE2, and CSF1R, with IC50 values of 100, 23, and 235 nM respectively. The compound enhances the tumor immune microenvironment through inhibition of angiogenesis and modulation of macrophage function. SJ-C1044 is applicable for research in colorectal cancer.

MDK5466 is an Flt3 inhibitor that acts by preventing glutamate-induced cell death.

Gersizangitide is an angiogenesis inhibitor.

Regorafenib (BAY 73-4506) mesylate is an orally active multi-target receptor tyrosine kinase inhibitor, inhibiting VEGFR1/2/3 (IC50=13/4.2/46 nM), PDGFRβ (IC50: 22 nM), Kit (IC50: 7 nM), RET (IC50: 1.5 nM), and Raf-1 (IC50: 2.5 nM), with potent anti-tumor and anti-angiogenic effects.

CEP-14083 is a potent ALK inhibitor that has shown activity in an NPM/ALK–carrying T-cell lymphoma in vitro study. Presumably, this compound binds to the hinge region of the kinase in an ATP-competitive manner. CEP-14083 displays a potent activity against ALK in enzymatic assays (IC50 = 11 nmol/L). Further, CEP-14083 is also able to inhibit the insulin receptor at a concentration within a nanomolar range. In a preclinical assay, CEP-14083 showed that, via NPM/ALK TK inhibition, it could control the expression of molecules that determine T-cell identity and signaling in lymphoma cells. CEP-14083 has shown preclinical activity in both cell lines and animal models harboring ALK alteration.

CEP-11981 is an orally active TIE2/pan-VEGFR inhibitor with broad tyrosine kinase inhibitory activity, exhibiting antitumour and anti-angiogenic effects, and is applicable for the treatment of refractory solid tumours.

Vanucizumab is a bispecific humanised monoclonal antibody that simultaneously inhibits the receptor interactions of VEGF-A and Angiopoietin-2 (Ang-2), exhibiting anti-angiogenic and anti-cancer effects, and can be used for the treatment of advanced solid tumours.

Zansecimab (LY-3127804) is a monoclonal antibody targeting angiopoietin 2 (Ang 2) for the study of cardiovascular and immune diseases.