tie-2

Altiratinib (DCC-2701)(DCC-2701) is a novel c-MET/TIE-2/VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with an HGF antagonist in vitro.

BAY-826 is a novel, potent and selective TIE-2 inhibitor that inhibits TIE-2 phosphorylation and can be used to study tumors.

EOC317 (ACTB-1003) is an oral kinase inhibitor with IC50 values of 6 nM, 2 nM, and 4 nM for FGFR1, VEGFR2, and Tie-2, respectively.

GSK-1070916 (GSK-1070916A) is a reversible and ATP-competitive inhibitor of Aurora B C with IC50 of 3.5 nM 6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1.

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].

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.

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.

Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

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

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

5α-Hydroxycostic acid, a naturally occurring sesquiterpene, inhibits choroidal neovascularization in rats through dual signaling pathways mediated by VEGF VEGFR and Ang2 Tie2 (angiopoietin 2), and exhibits anti-inflammatory and anti-angiogenic effects on human breast cancer cells

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.

Razuprotafib (AKB-9778) is a protein tyrosine phosphatase ß (HPTPß) inhibitor with an IC50 of 50 nM. It effectively activates Tie-2 and provides protection against acute kidney injury.

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).

Pexmetinib (ARRY-614) is an orally bioavailable dual p38 MAPK Tie-2 inhibitor studied in acute myeloid leukemia and inhibits osteoclastogenesis and breast cancer-induced osteolysis via the P38 STAT3 signaling pathway.

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.