Tie Inhibitor

Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC₅₀s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.

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.

Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. 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.

AMG-780 is a fully human IgG2 antibody that targets angiopoietin 1 (Ang1) (IC₅₀ = 4.5 nM) and angiopoietin 2 (Ang2) (IC₅₀ = 0.06 nM). AMG-780 inhibits tumor growth in the Colo205 xenograft mouse model by inhibiting both Ang1 and Ang2. AMG-780 is indicated for the research of cancers such as colon cancer.

Tie2 kinase inhibitor 3 (compound 63) is a potent Tie-2 kinase inhibitor with good oral activity (IC₅₀=30 nM). Tie2 kinase inhibitor 3 inhibits phosphorylation and signaling of Tie-2 by competing with the ATP binding site of Tie-2 kinase. This inhibition affects the stability and maturity of blood vessels, which has an impact on tumor angiogenesis. Tie2 kinase inhibitor 3 can be used to restrict tumor growth and regulate angiogenesis.

UBX2050 is a human monoclonal antibody (mAb) targeting TIE2. UBX2050 can be used in Age-related macular degeneration, Diabetic macular oedema and Diabetic retinopathy research.

DX-2240 is a human monoclonal antibody (mAb) targeting TIE1. DX-2240 inhibits tumor growth and sensitizes tumor vasculature to anti-angiogenic agents (VEGF pathway inhibitors).

Pexmetinib (Standard) is the analytical standard of Pexmetinib. This product is intended for research and analytical applications. Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.

Tie2 kinase inhibitor 1 (Standard) is the analytical standard of Tie2 kinase inhibitor 1 (HY-100556). This product is intended for research and analytical applications. 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.

Regorafenib (Standard) is the analytical standard of Regorafenib. This product is intended for research and analytical applications. 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.

CEP-14083 is a ATP-competitive ALK kinase inhibitor with an IC₅₀ value in enzymatic assays of 2 nM. CEP-14083 also inhibits other kinases, such as insulin receptor (IR), vascular endothelial growth factor receptor 2 (VEGFR2), angiopoietin-1 receptor (TIE2) and dual leucine zipper kinase (DLK). CEP-14083 suppresses CD274 mRNA expression and the NPM/ALK function in the NPM/ALK-carrying T cell lymphoma (ALK+TCL) cells. CEP-14083 is promising for research of lymphoma.