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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:8
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
Mouse TIE2, Fc Tag (Cat. No. ) 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.

Bioactivity-ELISA
Mouse TIE2, Fc TagMouse TIE2, Fc Tag (Cat. No. TI2-M5253) ELISA bioactivity

Immobilized Mouse Angiopoietin-2, His Tag (Cat. No. AN2-M52H3) at 5 μg/mL (100 μL/well) can bind Mouse TIE2, Fc Tag (Cat. No. TI2-M5253) with a linear range of 5-78 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
Ponatinib Hydrochloride AP24534 hydrochloride; AP24534-HCL; AP24534 HCl; INCB-84344; AP-24534 Approved Ariad Iclusig Japan Precursor Cell Lymphoblastic Leukemia-Lymphoma; Leukemia, Myelogenous, Chronic, BCR-ABL Positive Otsuka Holdings Co Ltd 2012-12-14 Precursor Cell Lymphoblastic Leukemia-Lymphoma; Carcinoma, Non-Small-Cell Lung; Leukemia, Biphenotypic, Acute; Lymphoma; Leukemia, Myeloid, Acute; Leukemia, Myeloid, Chronic-Phase; Gastrointestinal Stromal Tumors; Philadelphia Chromosome; Medullary thyroid cancer (MTC); Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Blast Crisis; Small Cell Lung Carcinoma; Adenocarcinoma of Lung; Solid tumours; Leukemia, Myeloid, Accelerated Phase; Leukemia; Hematologic Neoplasms Details
Ripretinib DCC-2618 Approved Deciphera 擎乐, Qinlock United Kingdom 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 Mainland China Gastrointestinal Stromal Tumors Bayer Pharma Ag 2012-09-27 Leukemia, Myeloid, Acute; Sarcoma; Gastrinoma; Colorectal Neoplasms; Gastrointestinal Stromal Tumors; Bile Duct Neoplasms; Peritoneal Neoplasms; Lymphoma, Non-Hodgkin; Lung Neoplasms; Carcinoma, Adenoid Cystic; Thyroid Neoplasms; Fallopian Tube Neoplasms; Carcinoma, Hepatocellular; Melanoma; Neoplasm Metastasis; Gastrointestinal Neoplasms; Somatostatinoma; Solid tumours; Glucagonoma; Multiple Myeloma; Pancreatic Neoplasms; Carcinoma, Ovarian Epithelial; Carcinoma, Transitional Cell; Neoplasms; Glioblastoma; Colonic Neoplasms; Hemangiosarcoma; Carcinoma, Islet Cell; Insulinoma; Carcinoid Tumor; Rectal Neoplasms; Carcinoma, Renal Cell; Ovarian Neoplasms Details
Cabozantinib S-malate XL-184; BMS-907351 Approved Exelixis Inc Cometriq, Cabometyx Japan Carcinoma, Renal Cell Takeda 2012-11-29 Thyroid Neoplasms; Adenocarcinoma, Follicular; Brain Neoplasms; Sarcoma; Neuroblastoma; Neurofibroma, Plexiform; Prostatic Neoplasms; Cholangiocarcinoma; Colorectal Neoplasms; Astrocytoma; Hepatic Insufficiency; Bile Duct Neoplasms; Central Nervous System Neoplasms; Lymphoma; Leukemia, Myeloid, Acute; Glioma; Carcinoma, Neuroendocrine; Carcinoma, Hepatocellular; Neoplasms, Germ Cell and Embryonal; Carcinoma, Non-Small-Cell Lung; Adenocarcinoma; Thyroid Cancer, Papillary; Meningioma; Carcinoma, Transitional Cell; Kidney Neoplasms; Ovarian germ cell tumor; Bone metastases; Carcinoma, Renal Cell; Rejection of liver transplantation; Esophageal Neoplasms; Pain; Stomach Neoplasms; Carcinoma, Merkel Cell; Glioblastoma; Seminoma; Solid tumours; Neurofibromatoses; Neoplasms; Salivary Gland Neoplasms; Carcinoma, Papillary; Skin Neoplasms; Kidney Diseases; Neuroendocrine Tumors; Adrenocortical Carcinoma; Prostatic Neoplasms, Castration-Resistant; Multiple Myeloma 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
Gersizangitide AXT-107 AsclepiX Therapeutics Inc Details
Altiratinib DP-5164; DCC-2701; DCC-22701; T-678746713 Deciphera Details
Trebananib AMG-386; 20060439 Amgen Inc, Takeda Pharmaceutical Co Ltd Details
Pexmetinib ARRY-614 Array Biopharma Details
Razuprotafib AKB-9778 Akebia Therapeutics Inc Details
Rebastinib Tosylate DP-1919; DCC-2036; DP-1919.TO Deciphera Details
QBH-196 QBH-196 Phase 1 Clinical Shenyang Pharmaceutical University Solid tumours; Stomach Neoplasms Details
Sitravatinib IND-155305; MG-516; MG-91516; MGCD-516 Phase 3 Clinical Mirati Therapeutics Ureteral Neoplasms; Melanoma; Gastrointestinal Neoplasms; Carcinoma, Non-Small-Cell Lung; Carcinoma, Hepatocellular; Lung Neoplasms; Mouth Neoplasms; Carcinoma, Squamous Cell; Endometrial Neoplasms; Esophageal Squamous Cell Carcinoma; Hepatic Insufficiency; Solid tumours; Breast Neoplasms; Liposarcoma; Lung Diseases; Triple Negative Breast Neoplasms; Carcinoma, Transitional Cell; Neoplasms; Carcinoma, Renal Cell; Carcinoma; Squamous Cell Carcinoma of Head and Neck; Biliary Tract Neoplasms Details

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