Tie

Angiopoietin receptor

Angiopoietins (Angs) are important vascular growth factors that regulate vascular remodeling, maturation, and stabilization. Angs also regulate vascular reactivity through regulating the production of nitric oxide (NO). The Angs family includes Ang1, Ang2, and Ang4 (a human orthologue of mouse Ang3) which interacts with tyrosine kinase receptors (Tie1 and Tie2). The angiopoietins receptors Tie1 and Tie2 (also known as TEK) are almost exclusively expressed in the endothelium, but there is some expression also in haematopoietic cells. The growth factors Ang1, Ang2 and Ang4 (the human orthologue of mouse Ang3) are ligands for Tie2, whereas Tie1 is an orphan receptor that can nevertheless be activated by angiopoietins via its interaction with Tie2. Ang-Tie signaling is involved in various processes of vascular development and remodeling in different diseases.

Tie Related Products (18):

By Effects:	Inhibitors (17) Activator (1)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-10331

Regorafenib	Inhibitor	99.93%
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/Flt-1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.

HY-109041

Razuprotafib	Activator	≥98.0%
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC₅₀of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC₅₀ of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC₅₀=36 pM) and HPTPγ (100 pM).

HY-10331A

Regorafenib monohydrate	Inhibitor	99.96%
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/Flt-1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.

HY-108333

SB-633825	Inhibitor	98.52%
SB-633825 is a potent and ATP-competitive inhibitor of TIE2, LOK (STK10) and BRK with IC₅₀s of 3.5 nM, 66 nM, 150 nM, respectively. SB-633825 can inhibit cancer cell growth and angiogenesis.

HY-100756

BAY-826	Inhibitor	99.94%
BAY-826 is a selective and potent TIE-2 inhibitor with a K_d of 1.6 nM, respectively.

HY-P99330

Vanucizumab	Inhibitor
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.

HY-112423

CE-245677	Inhibitor	98.14%
CE-245677 is a potent reversible inhibitor of Tie2 and TrkA/B kinases with a cellular IC₅₀s of 4.7 and 1 nM.

HY-100394

NVP-BAW2881	Inhibitor	98.17%
NVP-BAW2881 (BAW2881) is a potent and selective VEGFR2/KDR/Flk-1 inhibitor with an IC₅₀ of 4 nM.

HY-12572

TIE-2/VEGFR-2 kinase-IN-2	Inhibitor	99.79%
TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2/KDR/Flk-1 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.

HY-125741

GW768505A free base	Inhibitor	98.66%
GW768505A free base is a potent dual inhibitor of VEGFR2/KDR/Flk-1 (VEGFR2/KDR/Flk-1) and Tie-2, with a pIC₅₀ of 7.81 for VEGFR2/KDR/Flk-1. GW768505A free base has anti-angiogenic activity。

HY-112294

TIE-2/VEGFR-2 kinase-IN-1	Inhibitor	99.91%
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.

HY-10331B

Regorafenib mesylate	Inhibitor
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/Flt-1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity.

HY-P99510

Zansecimab	Inhibitor
Zansecimab (LY-3127804) is an immunoglobulin G4-kappa, a monoclonal antibody against angiopoietin 2 (Ang 2). Zansecimab has potential applications in angiogenesis and immune regulation.

HY-112475

Flt-3 Inhibitor III	Inhibitor
Flt-3 Inhibitor III is a potent and selective FLT3 kinase inhibitor with an ₅₀ of 50 nM. Flt-3 Inhibitor III shows less active against other kinases. Flt-3 Inhibitor III has anticancer effects.

HY-156638

TIE-2/VEGFR-2 kinase-IN-5	Inhibitor
TIE-2/VEGFR-2 kinase-IN-5 is an anti-angiogenic agent. TIE-2/VEGFR-2 kinase-IN-5 also is a potent TIE-2 and VEGFR-2 tyrosine kinase inhibitor with pIC₅₀ values of 7.78 nM and 8.11 nM, respectively. TIE-2/VEGFR-2 kinase-IN-5 can be used for the research of angiogenesis.

HY-156635

TIE-2/VEGFR-2 kinase-IN-3	Inhibitor
TIE-2/VEGFR-2 kinase-IN-3, benzimidazole, is a potent TIE-2 and VEGFR-2 tyrosine kinase receptors inhibitors with IC₅₀ values of 6.9 nM and 3.5 nM, respectively. TIE-2/VEGFR-2 kinase-IN-3 can be used for the research of angiogenesis.

HY-156637

TIE-2/VEGFR-2 kinase-IN-4	Inhibitor
TIE-2/VEGFR-2 kinase-IN-4, benzimidazole, is a potent TIE-2 and VEGFR-2 tyrosine kinase receptors inhibitors with IC₅₀ values of 5.2 nM and 5.1 nM, respectively. TIE-2/VEGFR-2 kinase-IN-4 can be used for the research of angiogenesis.

HY-113571

Tie2 kinase inhibitor 2	Inhibitor
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.

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