Tie2

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.

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.

AMG-Tie2-1 is a potent inhibitor of endothelial endothelial cell kinase 2 (Tie2) and VEGFR2 with anticancer and antitumor activity that affects cardiovascular production, and may be used in the study of cardiovascular disease and cancer.

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.

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.

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).

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.

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

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

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.

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.

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.

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].

Anti-TIE2/CD202b Antibody is a specific monoclonal antibody targeting the receptor tyrosine kinase TIE2 (CD202b). By binding to the TIE2 extracellular domain, it interferes with angiopoietin-mediated signaling, playing a critical role in regulating vascular development and tumor angiogenesis.

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.

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.

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.

NVP-BAW2881 (BAW2881) is a potent and selective VEGFR (vascular endothelial growth factor receptor tyrosine kinase) inhibitor with efficacy in inhibiting chronic and acute skin inflammation.

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-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.