Tie Inhibitor

Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC₅₀ values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.

Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor, with IC₅₀ values of 0.8 nM and 4 nM against Abl1^WT and Abl1^T315I, respectively. Rebastinib potently inhibits CYP2C8 (IC₅₀ = 0.0533 μM) and CYP2C9 (IC₅₀ = 2.54 μM). Rebastinib allosterically inhibits Tie2 with an IC₅₀ of 0.63 nM. Rebastinib inhibits the transcriptional activity of FoxO1. Rebastinib inhibits SRC family kinases, KDR and FLT3 kinases. Rebastinib induces Apoptosis. Rebastinib exerts anti-tumor activity in breast cancer. Rebastinib exerts anti-angiogenic effects. Rebastinib increases myotube diameter and improves reduced contractility. Rebastinib can be used in research related to triple-negative breast cancer, luminal breast cancer, pancreatic neuroendocrine tumors, muscle atrophy, cancer cachexia, chronic myeloid leukemia, and B-lymphocytic leukemia.

Pexmetinib (ARRY-614) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib binds to Tie-2 and p38 MAPK in a "DFG-out" conformation, attenuates the phosphorylation of p38, inhibits STAT3 activation, reduces the promoter-binding activity of NFATc1, and decreases the expression of MMPs. Pexmetinib inhibits leukemia cell proliferation, abrogates TNF-α-mediated myelosuppression of healthy hematopoietic stem cells, stimulates hematopoiesis in primary myelodysplastic syndrome (MDS) samples, inhibits RANKL-induced osteoclast formation and bone resorption, and suppresses migration, invasion and induced osteolysis of breast cancer cells. Pexmetinib can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis.

Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC₅₀ values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.

CEP-14513 is an ALK inhibitor with an IC₅₀ of 4 nM. CEP-14513 also inhibits insulin receptor, VEGFR2, TIE2 and DLK kinases, but does not inhibit MET, IKKβ, or CDK1/2/5. CEP-14513 induces cancer cell apoptosis. CEP-14513 is applicable to research related to non-small cell lung cancer, anaplastic large cell lymphoma, inflammatory myofibroblastic tumor, and diffuse large B-cell lymphoma.

Rebastinib tosylate (DCC-2036 tosylate) is an orally active, non-ATP-competitive Bcr-Abl inhibitor, with IC₅₀ values of 0.8 nM and 4 nM against Abl1^WT and Abl1^T315I, respectively. Rebastinib tosylate potently inhibits CYP2C8 (IC₅₀ = 0.0533 μM) and CYP2C9 (IC₅₀ = 2.54 μM). Rebastinib tosylate allosterically inhibits Tie2 with an IC₅₀ of 0.63 nM. Rebastinib tosylate inhibits the transcriptional activity of FoxO1. Rebastinib tosylate inhibits SRC family kinases, KDR and FLT3 kinases. Rebastinib tosylate induces Apoptosis. Rebastinib tosylate exerts anti-tumor activity in breast cancer. Rebastinib tosylate exerts anti-angiogenic effects. Rebastinib tosylate increases myotube diameter and improves reduced contractility. Rebastinib tosylate can be used in research related to triple-negative breast cancer, luminal breast cancer, pancreatic neuroendocrine tumors, muscle atrophy, cancer cachexia, chronic myeloid leukemia, and B-lymphocytic leukemia.

Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC₅₀ of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.

BAY-826, a chemical probe, is a selective and potent TIE-2 inhibitor with a K_d of 1.6 nM, respectively.

Nesvacumab is a fully human immunoglobulin G1 (IgG1) monoclonal antibody that specifically binds and inactivates the Tie2 receptor ligand Angiopoietin-2 (Ang2) with high affinity, but shows no binding to Ang1. Nesvacumab can be used in vascular researches.

Vanucizumab is a first-in-class, bispecific IgG1-like monoclonal antibody that simultaneously blocks VEGF-A and angiopoietin-2 (Ang-2) from interacting with their receptors. Vanucizumab has antiangiogenic and anticancer effects.

Trebananib (2xCon4C) is an Fc fusion peptibody. Trebananib exerts its effects by blocking the binding of angiopoietin 1 (Ang1) and angiopoietin 2 (Ang2) to the TIE2 receptor. Trebananib has anti-angiogenic and anti-tumor activities.

Zansecimab (LY-3127804) is a monoclonal antibody against angiopoietin 2 (Ang‑2). Zansecimab can be used in research on angiogenesis, immunomodulation and anti-tumor activity.

TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC₅₀ values of 8.61 and 8.56, respectively. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research.

NVP-BAW2881 (BAW2881) is a potent and selective VEGFR2 inhibitor with an IC₅₀ of 9 nM.

Tie2 kinase inhibitor 2 (compound 7) is a selective Tie2 kinase inhibitor with an IC₅₀ value of 1 μM. Tie2 kinase inhibitor 2 inhibits endothelial cell tube formation, and can be used for Tie2-mediated angiogenic disorders research.

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

CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC₅₀s of 4.7 and 1 nM.

TIE-2/VEGFR-2 kinase-IN-1 is used for the synthesis of TIE-2 and/or VEGFR-2 inhibitors, extracted from patent WO2003022852, example 14. TIE-2/VEGFR-2 kinase-IN-1 is used for the study of diseases associated with inappropriate angiogenesis.

RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R and Tie-2 with IC₅₀ values of 0.24, 1.19, 10.74 and 5.85 µM, respectively. RK-20448 also inhibits BLK, Csk, Fyn and Lyn with IC₅₀ values of 0.37, 4.27, 2.03 and 0.43 µM, respectively. RK-20448 is the cis isomer of A-419259 (HY-15764).

Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC₅₀ values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity.