tie-2

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.

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.

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-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].

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].

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

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

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.

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.

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.

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.

DCC-2036 (Rebastinib (DCC-2036)) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC, HCK, FGR, FLT3, KDR, and Tie-2, and low activity to c-Kit. Rebastinib aimed at the Angiopoietin2-Tie2 pathway.

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

LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 (KDR), PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. In vivo, LY2457546 inhibited VEGF-driven autophosphorylation of lung KDR in the mouse and rat in a dose and concentration dependent manner. LY2457546 was well tolerated and exhibited efficacy in a 13762 syngeneic rat mammary tumor models. Additionally, LY2457546 caused complete regression of well-established tumors in an acute myelogenous leukemia (AML) FLT3-ITD mutant xenograft tumor model. The unique spectrum of target activity, potent in vivo anti-tumor efficacy in a variety of rodent and human solid tumor models, exquisite potency against a clinically relevant model of AML, and non-clinical safety profile justify the advancement of LY2457546 into clinical testing. (source: Invest New D......

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).

RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR VEGF2R, and Tie-2. It also inhibits BLK, Csk, Fyn, and Lyn. RK-20448 is the cis isomer of A-419259

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.

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.

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.

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.

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.