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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:10
Lastest Research Phase:Approved

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Part of Bioactivity data

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).

TI2-M5253-MALS-HPLC
TIE2 MALS images

The purity of Mouse TIE2, Fc Tag (Cat. No. TI2-M5253) is more than 90% and the molecular weight of this protein is around 235-285kDa 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
Cabozantinib S-malate XL-184; BMS-907351 Approved Exelixis Inc Cometriq, Cabometyx United States Carcinoma, Neuroendocrine; Thyroid Neoplasms Exelixis Inc 2012-11-29 Carcinoma, Adenosquamous; Uterine Neoplasms; Thyroid Neoplasms; Hepatic Insufficiency; Gliosarcoma; Bile Duct Neoplasms; Peritoneal Neoplasms; Astrocytoma; Colorectal Neoplasms; Brain Neoplasms; Endometrial Neoplasms; Osteosarcoma; Urethral Neoplasms; Adenocarcinoma, Clear Cell; Neuroblastoma; Neurofibroma, Plexiform; Cholangiocarcinoma; Medullary thyroid cancer (MTC); Sarcoma, Ewing; Breast Neoplasms; Carcinoma, Endometrioid; Neoplasms, Germ Cell and Embryonal; Meningioma; Melanoma; Adenocarcinoma; Carcinoma, Non-Small-Cell Lung; Thyroid Cancer, Papillary; Neoplasm Metastasis; Paraganglioma; Carcinoma, Hepatocellular; Sarcoma, Clear Cell; Carcinoma, Neuroendocrine; Fallopian Tube Neoplasms; Brain metastases; Lymphoma; Leukemia, Myeloid, Acute; Sarcoma, Alveolar Soft Part; Glioma; Carcinoma, Squamous Cell; Pain; Adrenal Cortex Neoplasms; Pancreatic neuroendocrine tumors (pNET); Glioblastoma; Kidney Diseases; Hepatoblastoma; Pheochromocytoma; Carcinoma, Renal Cell; Rejection of liver transplantation; Carcinoid Details
Ponatinib Hydrochloride AP24534 hydrochloride; AP24534-HCL; AP24534 HCl; INCB-84344; AP-24534 Approved Ariad Iclusig United States Precursor Cell Lymphoblastic Leukemia-Lymphoma; Leukemia, Myelogenous, Chronic Ariad Pharmaceuticals Inc 2012-12-14 Precursor Cell Lymphoblastic Leukemia-Lymphoma; Leukemia, Biphenotypic, Acute; Carcinoma, Non-Small-Cell Lung; Thyroid Neoplasms; Lymphoma; Leukemia, Myeloid, Acute; Gastrointestinal Stromal Tumors; Leukemia, Myeloid, Chronic-Phase; Philadelphia Chromosome; Common Bile Duct Neoplasms; Precursor T-Cell Lymphoblastic Leukemia-Lymphoma; Medullary thyroid cancer (MTC); Leukemia, Myelogenous, Chronic; Blast Crisis; Glioblastoma; Leukemia, Myelomonocytic, Chronic; Adenocarcinoma of Lung; Neoplasms; Small Cell Lung Carcinoma; Solid tumours; Hematologic Neoplasms; Leukemia, Myeloid, Accelerated Phase; Leukemia; Head and Neck Neoplasms Details
Ripretinib DCC-2618 Approved Deciphera Qinlock, 擎乐 United States Gastrointestinal Stromal Tumors Deciphera Pharmaceuticals Llc 2020-05-15 Neoplasms; Mastocytosis, Systemic; Gastrointestinal Stromal Tumors Details
Regorafenib DAST; BAY-73-4506 Approved Bayer AG Stivarga, Resihance United States Colorectal Neoplasms Bayer Healthcare Pharmaceuticals Inc 2012-09-27 Esophageal adenocarcinoma; Osteosarcoma; Sarcoma, Ewing; Bile Duct Neoplasms; Peritoneal Neoplasms; Bone Neoplasms; Colorectal Neoplasms; Gastrointestinal Stromal Tumors; Fallopian Tube Neoplasms; Lung Neoplasms; Thyroid Neoplasms; Sarcoma; Leukemia, Myeloid, Acute; Thymoma; Melanoma; Gastrointestinal Neoplasms; Carcinoma, Hepatocellular; Adenocarcinoma; Somatostatinoma; Neoplasm Metastasis; Carcinoma, Non-Small-Cell Lung; Carcinoma, Ovarian Epithelial; Solid tumours; Liver Neoplasms; Carcinoid Tumor; Esophageal Neoplasms; Stomach Neoplasms; Carcinoma, Islet Cell; Insulinoma; Hemangiosarcoma; Rectal Neoplasms; Carcinoma, Renal Cell; Ovarian Neoplasms; Pancreatic Neoplasms; Colonic Neoplasms; Neoplasms; Glioblastoma; Carcinoma, Transitional Cell; Glucagonoma; Carcinoma, Adenoid Cystic; Adenoma; Gastrinoma Details

Clinical Drug Information

Name Research Code Research Phase Company Indications Clinical Trials
Merestinib 5OGS5K699E; LY-2801653 Phase 2 Clinical Eli Lilly And Company Biliary Tract Neoplasms; Skin Melanoma; Bone metastases; Solid tumours; Neoplasms; Pancreatic Neoplasms; Microsatellite instability-high cancer; Breast Neoplasms; Lymphoma, Mantle-Cell; Cholangiocarcinoma; Colorectal Neoplasms; Leukemia, Myeloid, Acute; Lymphoma, Non-Hodgkin; Gallbladder Neoplasms; Neoplasm Metastasis; Carcinoma, Non-Small-Cell Lung Details
Glesatinib MGCD-265; MG-90265X; 7Q29OXD98N; MG-90265H9; MG-90265gly; MG-90265 Phase 2 Clinical Mirati Therapeutics Inc Neoplasms; Carcinoma, Non-Small-Cell Lung Details
QBH-196 QBH-196 Phase 1 Clinical Shenyang Pharmaceutical University Solid tumours; Stomach Neoplasms Details
AV-001 AV-001 Phase 2 Clinical Vasomune Therapeutics Inc Respiratory Tract Infections; Pneumonia; Coronavirus Disease 2019 (COVID-19); Respiratory Distress Syndrome, Adult; Pneumonia, Viral Details
PMC-403 PMC-403 Phase 1 Clinical Pharmabcine Capillary Leak Syndrome; Solid tumours; Wet Macular Degeneration; Macular Degeneration Details
Razuprotafib AKB-9778 Phase 2 Clinical Akebia Therapeutics Inc Coronavirus Disease 2019 (COVID-19); Respiratory Distress Syndrome, Adult; Glaucoma, Open-Angle; Ocular Hypertension; Diabetic macular oedema; Diabetic Retinopathy; Retinal Vein Occlusion Details
Trebananib AMG-386; 20060439 Phase 2 Clinical Amgen Inc, Takeda Pharmaceutical Co Ltd Lung Neoplasms; Prostatic Neoplasms; Brain Neoplasms; Sarcoma; Carcinoma, Adenosquamous; Peritoneal Neoplasms; Colorectal Neoplasms; Genital Neoplasms, Female; Gliosarcoma; Fallopian Tube Neoplasms; Breast Neoplasms; Uterine Neoplasms; Leukemia, Monocytic, Acute; Leukemia, Myeloid, Acute; Endometrial Neoplasms; Neoplasm Metastasis; Gastrointestinal Neoplasms; Carcinoma, Non-Small-Cell Lung; Adenocarcinoma; Colonic Neoplasms; Solid tumours; Leukemia, Myeloid; Leukemia, Erythroblastic, Acute; Carcinoma; Rectal Neoplasms; Carcinoma, Renal Cell; Hemangiosarcoma; Neoplasms; Ovarian Neoplasms; Kidney Diseases; Glioblastoma; Leukemia, Myelomonocytic, Acute; Central Nervous System Neoplasms; Neuroendocrine Tumors; Leukemia, Megakaryoblastic, Acute; Oligodendroglioma; Sarcoma, Endometrial Stromal Details
CEP-11981 ESK-981; CEP-11981; SSR-106462; BOL-303213X Phase 2 Clinical Sanofi Neoplasms; Adenoma, Islet Cell; Pancreatic Neoplasms; Prostatic Neoplasms, Castration-Resistant; Prostatic Neoplasms; Carcinoma, Adenosquamous; Carcinoma, Neuroendocrine; Gastrointestinal Neoplasms Details
Gersizangitide AXT-107 Phase 2 Clinical AsclepiX Therapeutics Inc Diabetic macular oedema; Macular Degeneration Details
Rebastinib Tosylate DP-1919; DCC-2036; DP-1919.TO Phase 2 Clinical Deciphera Leukemia, Myelogenous, Chronic; Solid tumours Details

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