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Your Position: Home > TIE2

TIE2

Brief Information

Name:TEK receptor tyrosine kinase
Target Synonym:EC:2.7.10.1,Endothelial Tyrosine Kinase,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,TEK Tyrosine Kinase, Endothelial,VMCM1,VMCM,TIE2,Venous Malformations, Multiple Cutaneous And Mucosal,CD202b Antigen,EC 2.7.10.1,CD202B,GLC3E,TIE-2,HTIE2,Receptor, TIE-2,EC 2.7.10
Number of Launched Drugs:4
Number of Drugs in Clinical Trials:8
Lastest Research Phase:Approved

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Cat. No. Species Product Description Structure Purity Feature
TI2-M52H3 Mouse Mouse TIE2 Protein, His Tag (MALS verified)
TI2-M52H3-structure
TI2-M52H3-sds
TI2-H52H3 Human Human TIE2 Protein, His Tag (MALS verified)
TI2-H52H3-structure
TI2-H52H3-sds
TI2-M5253 Mouse Mouse TIE2 Protein, Fc Tag (MALS verified)
TI2-M5253-structure
TI2-M5253-sds
TI2-C5253 Cynomolgus Cynomolgus TIE2 Protein, His Tag (MALS verified)
TI2-C5253-structure
TI2-C5253-sds
TI2-H5255 Human Human TIE2 Protein, Fc Tag (MALS verified)
TI2-H5255-structure
TI2-H5255-sds
ACRO Quality

Part of Bioactivity data

TI2-H52H3-ELISA
TIE2 ELISA

Immobilized Human TIE2 Protein, His Tag (Cat. No. TI2-H52H3) at 2 μg/mL (100 μL/well) can bind Biotinylated Human Angiopoietin-2 Protein, His,Avitag (Cat. No. AN2-H82E9) with a linear range of 5-78 ng/mL (QC tested).

Protocol
TI2-M52H3-MALS-HPLC
TIE2 MALS images

The purity of Mouse TIE2 Protein, His Tag (Cat. No. TI2-M52H3) is more than 85% and the molecular weight of this protein is around 90-125 kDa verified by SEC-MALS.

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 DAST; BAY-73-4506 Approved Bayer AG Stivarga, Resihance United States Colorectal Neoplasms Bayer Healthcare Pharmaceuticals Inc 2012-09-27 Leukemia, Myeloid, Acute; Sarcoma, Ewing; Colorectal Neoplasms; Gastrointestinal Stromal Tumors; Bone Neoplasms; Peritoneal Neoplasms; Bile Duct Neoplasms; Esophageal adenocarcinoma; Lung Neoplasms; Thyroid Neoplasms; Fallopian Tube Neoplasms; Osteosarcoma; Thymoma; Carcinoma, Non-Small-Cell Lung; Carcinoma, Hepatocellular; Neoplasm Metastasis; Adenocarcinoma; Somatostatinoma; Gastrointestinal Neoplasms; Melanoma; Meningioma; Neoplasms; Solid tumours; Liver Neoplasms; Stomach Neoplasms; Esophageal Neoplasms; Insulinoma; Carcinoma, Islet Cell; Hemangiosarcoma; Rectal Neoplasms; Carcinoma, Renal Cell; Ovarian Neoplasms; Colonic Neoplasms; Carcinoma, Ovarian Epithelial; Pancreatic Neoplasms; Carcinoma, Transitional Cell; Adenoma; Glucagonoma; Carcinoma, Adenoid Cystic; Gastrinoma; Sarcoma Details
Ripretinib DCC-2618 Approved Deciphera Pharmaceuticals Qinlock, 擎乐 United States Gastrointestinal Stromal Tumors Deciphera Pharmaceuticals Llc 2020-05-15 Mastocytosis, Systemic; Neoplasms; Gastrointestinal Stromal Tumors Details
Ponatinib Hydrochloride AP24534 hydrochloride; AP24534-HCL; AP24534 HCl; INCB-84344; AP-24534 Approved Ariad Iclusig United States Leukemia, Myelogenous, Chronic; Precursor Cell Lymphoblastic Leukemia-Lymphoma Ariad Pharmaceuticals Inc 2012-12-14 Precursor Cell Lymphoblastic Leukemia-Lymphoma; Carcinoma, Non-Small-Cell Lung; Leukemia, Biphenotypic, Acute; Thyroid Neoplasms; Lymphoma; Leukemia, Myeloid, Acute; Gastrointestinal Stromal Tumors; Leukemia, Myeloid, Chronic-Phase; Philadelphia Chromosome; Precursor T-Cell Lymphoblastic Leukemia-Lymphoma; Medullary thyroid cancer (MTC); Common Bile Duct Neoplasms; Leukemia, Myeloid, Accelerated Phase; Blast Crisis; Leukemia, Myelomonocytic, Chronic; Glioblastoma; Small Cell Lung Carcinoma; Adenocarcinoma of Lung; Hematologic Neoplasms; Head and Neck Neoplasms; Leukemia, Myelogenous, Chronic; Solid tumours; Leukemia Details
Cabozantinib S-malate XL-184; BMS-907351; RO7047650; RO-7047650 Approved Exelixis Inc Cometriq, Cabometyx United States Thyroid Neoplasms; Carcinoma, Neuroendocrine Exelixis Inc 2012-11-29 Neuroblastoma; Thyroid Neoplasms; Hepatic Insufficiency; Astrocytoma; Peritoneal Neoplasms; Bile Duct Neoplasms; Colorectal Neoplasms; Gliosarcoma; Urethral Neoplasms; Sarcoma, Clear Cell; Uterine Neoplasms; Cholangiocarcinoma; Neurofibroma, Plexiform; Brain Neoplasms; Adenocarcinoma, Clear Cell; Carcinoma, Adenosquamous; Medullary thyroid cancer (MTC); Sarcoma, Ewing; Sarcoma; Osteosarcoma; Sarcoma, Alveolar Soft Part; Meningioma; Melanoma; Neoplasm Metastasis; Carcinoma, Non-Small-Cell Lung; Carcinoma, Endometrioid; Thyroid Cancer, Papillary; Paraganglioma; Neoplasms, Germ Cell and Embryonal; Carcinoma, Hepatocellular; Prostatic Neoplasms; Glioma; Brain metastases; Endometrial Neoplasms; Leukemia, Myeloid, Acute; Carcinoma, Squamous Cell; Lymphoma; Carcinoma, Neuroendocrine; Fallopian Tube Neoplasms; Carcinoma, Renal Cell; Adenoma, Islet Cell; Glioblastoma; Carcinoma, Ovarian Epithelial; Renal Insufficiency; Hepatoblastoma; Pheochromocytoma; Carcinoid Tumor; Carcinoma, Merkel Cell; Rejection of liver transp Details

Clinical Drug Information

Name Research Code Research Phase Company Indications Clinical Trials
AV-001 (Vasomune Therapeutics) AV-001 (Vasomune Therapeutics) Phase 2 Clinical Sunnybrook Health Sciences Centre Respiratory Tract Infections; Pneumonia; Coronavirus Disease 2019 (COVID-19); Respiratory Distress Syndrome, Adult; Pneumonia, Viral Details
Razuprotafib AKB-9778; EYP-2301 Phase 2 Clinical Akebia Therapeutics Inc Coronavirus Disease 2019 (COVID-19); Glaucoma, Open-Angle; Respiratory Distress Syndrome, Adult; Ocular Hypertension; Diabetic macular oedema; Diabetic Retinopathy; Retinal Vein Occlusion Details
Merestinib 5OGS5K699E; LY-2801653 Phase 2 Clinical Eli Lilly And Company Biliary Tract Neoplasms; Solid tumours; Skin Melanoma; Bone metastases; Pancreatic Neoplasms; Neoplasms; Microsatellite instability-high cancer; Breast Neoplasms; Cholangiocarcinoma; Lymphoma, Mantle-Cell; Colorectal Neoplasms; Leukemia, Myeloid, Acute; Lymphoma, Non-Hodgkin; Gallbladder Neoplasms; Neoplasm Metastasis; Carcinoma, Non-Small-Cell Lung Details
Trebananib AMG-386; 20060439 Phase 2 Clinical Amgen Inc, Takeda Pharmaceutical Co Ltd Fallopian Tube Neoplasms; Carcinoma, Adenosquamous; Sarcoma; Breast Neoplasms; Brain Neoplasms; Prostatic Neoplasms; Peritoneal Neoplasms; Gliosarcoma; Genital Neoplasms, Female; Colorectal Neoplasms; Endometrial Neoplasms; Adenocarcinoma, Clear Cell; Leukemia, Monocytic, Acute; Leukemia, Myeloid, Acute; Lung Neoplasms; Uterine Neoplasms; Carcinoma, Endometrioid; Neoplasm Metastasis; Carcinoma, Hepatocellular; Carcinoma, Non-Small-Cell Lung; Gastrointestinal Neoplasms; Glioblastoma; Ovarian Neoplasms; Leukemia, Erythroblastic, Acute; Leukemia, Myeloid; Carcinoma, Renal Cell; Renal Insufficiency; Hemangiosarcoma; Rectal Neoplasms; Carcinoma; Leukemia, Myelomonocytic, Acute; Solid tumours; Carcinoma, Transitional Cell; Neoplasms; Colonic Neoplasms; Kidney Diseases; Sarcoma, Endometrial Stromal; Leukemia, Megakaryoblastic, Acute; Oligodendroglioma; Central Nervous System Neoplasms; Neuroendocrine Tumors Details
IGT-427 IGT-427 Phase 2 Clinical Ingenia Therapeutics Inc Retinal Diseases; Wet Macular Degeneration; Diabetic macular oedema Details
Gersizangitide AXT-107 Phase 2 Clinical AsclepiX Therapeutics Inc Diabetic macular oedema; Macular Degeneration Details
CEP-11981 ESK-981; CEP-11981; SSR-106462; BOL-303213X Phase 2 Clinical Sanofi Bone metastases; Neoplasms; Adenoma, Islet Cell; Pancreatic Neoplasms; Prostatic Neoplasms, Castration-Resistant; Carcinoma, Adenosquamous; Prostatic Neoplasms; Carcinoma, Neuroendocrine; Gastrointestinal Neoplasms Details
PMC-403 PMC-403 Phase 1 Clinical Pharmabcine Capillary Leak Syndrome; Solid tumours; Wet Macular Degeneration; Macular Degeneration Details
QBH-196 QBH-196 Phase 1 Clinical Shenyang Pharmaceutical University Solid tumours; Stomach Neoplasms Details

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