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TIE2

Brief Information

Name:TEK receptor tyrosine kinase
Target Synonym:EC 2.7.10,EC:2.7.10.1,Tyrosine-protein kinase receptor TEK,Tunica interna endothelial cell kinase,Angiopoietin-1 receptor,p140 TEK,Tyrosine kinase with Ig and EGF homology domains-2,TEK,TEK Receptor Tyrosine Kinase,Tyrosine-Protein Kinase Receptor TIE-2,T
Number of Launched Drugs:4
Number of Drugs in Clinical Trials:7
Lastest Research Phase:Approved

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By Product Status:
By Product Category:
By Conjugate:
Cat. No. Species Product Description Structure Purity Feature
TI2-M5253 Mouse Mouse TIE2 Protein, Fc Tag
TI2-M5253-structure
TI2-C5253 Cynomolgus Cynomolgus TIE2 Protein, His Tag
TI2-C5253-structure
TI2-H5255 Human Human TIE2 Protein, Fc Tag (MALS verified)
TI2-H5255-structure
TI2-H5255-sds
TI2-H5255-elisa_1

Part of Bioactivity data

TI2-H5255-MALS-HPLC
Human TIE2, Fc Tag (Cat. No. ) MALS images

The purity of Human TIE2, Fc Tag (Cat. No. TI2-H5255) was more than 90% and the molecular weight of this protein is around 250-270 kDa verified by SEC-MALS.

Bioactivity-ELISA
Human TIE2, Fc TagHuman TIE2, Fc Tag (Cat. No. TI2-H5255) ELISA bioactivity

Immobilized Biotinylated Human Angiopoietin-2, His,Avitag (Cat. No. AN2-H82E7) at 1 μg/mL (100 μL/well) on streptavidin (Cat. No. STN-N5116) precoated (0.5 μg/well) plate can bind Human TIE2, Fc Tag (Cat. No. TI2-H5255) with a linear range of 0.6-10 ng/mL (QC tested).

TI2-H5255-ELISA
Human TIE2, Fc TagHuman TIE2, Fc Tag (Cat. No. TI2-H5255) ELISA bioactivity

Immobilized Biotinylated Human Angiopoietin-2, His,Avitag (Cat. No. AN2-H82E7) at 1 μg/mL (100 μL/well) on streptavidin (Cat. No. STN-N5116) precoated (0.5 μg/well) plate can bind Human TIE2, Fc Tag (Cat. No. TI2-H5255) with a linear range of 0.6-10 ng/mL (QC tested).

Synonym Name

TIE2,Tie-2,TEK,VMCM, VMCM1,CD202b,Angiopoietin-1 receptor

Background

Tyrosine-protein kinase that acts as cell-surface receptor for ANGPT1, ANGPT2 and ANGPT4 and regulates angiogenesis, endothelial cell survival, proliferation, migration, adhesion and cell spreading, reorganization of the actin cytoskeleton, but also maintenance of vascular quiescence. Has anti-inflammatory effects by preventing the leakage of proinflammatory plasma proteins and leukocytes from blood vessels. Required for normal angiogenesis and heart development during embryogenesis. Required for post-natal hematopoiesis. After birth, activates or inhibits angiogenesis, depending on the context. Inhibits angiogenesis and promotes vascular stability in quiescent vessels, where endothelial cells have tight contacts. In quiescent vessels, ANGPT1 oligomers recruit TEK to cell-cell contacts, forming complexes with TEK molecules from adjoining cells, and this leads to preferential activation of phosphatidylinositol 3-kinase and the AKT1 signaling cascades. In migrating endothelial cells that lack cell-cell adhesions, ANGT1 recruits TEK to contacts with the extracellular matrix, leading to the formation of focal adhesion complexes, activation of PTK2/FAK and of the downstream kinases MAPK1/ERK2 and MAPK3/ERK1, and ultimately to the stimulation of sprouting angiogenesis. ANGPT1 signaling triggers receptor dimerization and autophosphorylation at specific tyrosine residues that then serve as binding sites for scaffold proteins and effectors. Signaling is modulated by ANGPT2 that has lower affinity for TEK, can promote TEK autophosphorylation in the absence of ANGPT1, but inhibits ANGPT1-mediated signaling by competing for the same binding site. Signaling is also modulated by formation of heterodimers with TIE1, and by proteolytic processing that gives rise to a soluble TEK extracellular domain. The soluble extracellular domain modulates signaling by functioning as decoy receptor for angiopoietins. TEK phosphorylates DOK2, GRB7, GRB14, PIK3R1; SHC1 and TIE1.

Clinical and Translational Updates

Public Drug Information

Name Research Code Research Phase Company First Brand Name First Approved Country First Indication First Approved Company First Approved Date Indications Clinical Trials
Regorafenib Monohydrate BAY-73-4506; DAST Approved Bayer Ag Stivarga, Resihance Mainland China Gastrointestinal Stromal Tumors Bayer Pharma Ag 2012-09-27 Solid tumours; Rectal Neoplasms; Carcinoma, Renal Cell; Colonic Neoplasms; Colorectal Neoplasms; Gastrointestinal Stromal Tumors; Carcinoma, Hepatocellular; Gastrointestinal Neoplasms Details
Vandetanib CH-331; ZD-6474; AZD-6474 Approved Astrazeneca Pharmaceutical Co Ltd Zactima, Caprelsa Japan Medullary thyroid cancer (MTC) Astrazeneca Pharmaceutical Co Ltd 2011-04-06 Solid tumours; Multiple Myeloma; Mesothelioma; Medullary thyroid cancer (MTC); Prostatic Neoplasms; Breast Neoplasms; Colorectal Neoplasms; Thyroid Neoplasms; Carcinoma, Neuroendocrine; Lung Neoplasms; Carcinoma, Non-Small-Cell Lung; Neoplasm Metastasis; Carcinoma, Hepatocellular Details
Ponatinib Hydrochloride AP-24534; INCB-84344; AP24534 HCl; AP24534-HCL; AP24534 hydrochloride Approved Ariad Iclusig Japan Precursor Cell Lymphoblastic Leukemia-Lymphoma; Leukemia, Myelogenous, Chronic, BCR-ABL Positive Otsuka Holdings Co Ltd 2012-12-14 Leukemia; Leukemia, Myeloid, Accelerated Phase; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Solid tumours; Hematologic Neoplasms; Blast Crisis; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Leukemia, Myeloid, Chronic-Phase; Philadelphia Chromosome; Gastrointestinal Stromal Tumors; Leukemia, Myeloid, Acute; Lymphoma; Leukemia, Biphenotypic, Acute Details
Cabozantinib S-malate BMS-907351; XL-184 Approved Exelixis Inc Cometriq, Cabometyx Japan Carcinoma, Renal Cell Takeda 2012-11-29 Solid tumours; Pain; Stomach Neoplasms; Carcinoma, Renal Cell; Esophageal Neoplasms; Glioblastoma; Kidney Diseases; Prostatic Neoplasms; Colorectal Neoplasms; Astrocytoma; Hepatic Insufficiency; Thyroid Neoplasms; Carcinoma, Neuroendocrine; Lymphoma; Carcinoma, Non-Small-Cell Lung; Carcinoma, Hepatocellular Details

Clinical Drug Information

Name Research Code Research Phase Company Indications Clinical Trials
CEP-11981 ESK-981; CEP-11981; SSR-106462; BOL-303213X Phase 2 Clinical Sanofi Prostatic Neoplasms Details
Altiratinib DP-5164; DCC-2701; DCC-22701; T-678746713 Phase 1 Clinical Deciphera Solid tumours; Neoplasms Details
Trebananib AMG-386; 20060439 Phase 2 Clinical Amgen Inc, Takeda Pharmaceutical Co Ltd Ovarian Neoplasms; Solid tumours; Carcinoma, Renal Cell; Carcinoma; Rectal Neoplasms; Kidney Diseases; Colonic Neoplasms; Breast Neoplasms; Peritoneal Neoplasms; Genital Neoplasms, Female; Colorectal Neoplasms; Fallopian Tube Neoplasms; Carcinoma, Non-Small-Cell Lung; Neoplasm Metastasis; Gastrointestinal Neoplasms Details
Rebastinib Tosylate DP-1919; DCC-2036; DP-1919.TO Phase 2 Clinical Deciphera Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Solid tumours; Leukemia, Lymphocytic, Chronic, B-Cell Details
Razuprotafib AKB-9778 Phase 2 Clinical Akebia Therapeutics Coronavirus Disease 2019 (COVID-19); Glaucoma, Open-Angle; Respiratory Distress Syndrome, Adult; Ocular Hypertension; Diabetic macular oedema; Retinal Vein Occlusion; Diabetic Retinopathy Details
AXT-107 AXT-107 Phase 2 Clinical AsclepiX Therapeutics Inc Diabetic macular oedema; Macular Degeneration Details
QBH-196 QBH-196 Phase 1 Clinical Shenyang Pharmaceutical University Stomach Neoplasms Details
Sitravatinib MG-516; MG-91516; MGCD-516; IND-155305 Phase 3 Clinical Mirati Therapeutics Solid tumours; Carcinoma; Carcinoma, Renal Cell; Carcinoma, Transitional Cell; Neoplasms; Hepatic Insufficiency; Ureteral Neoplasms; Carcinoma, Non-Small-Cell Lung; Gastrointestinal Neoplasms; Carcinoma, Hepatocellular Details

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