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TIE2

요약

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

제품 리스트 구매

일부의 생물활성 데이터

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).

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

공개 약품 정보

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 Blast Crisis; Carcinoma, Non-Small-Cell Lung; Leukemia, Biphenotypic, Acute; Thyroid Neoplasms; Lymphoma; Leukemia, Myeloid, Acute; Leukemia, Myeloid, Chronic-Phase; Gastrointestinal Stromal Tumors; Philadelphia Chromosome; Medullary thyroid cancer (MTC); Common Bile Duct Neoplasms; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Glioblastoma; Leukemia, Myelomonocytic, Chronic; Neoplasms; Small Cell Lung Carcinoma; Adenocarcinoma of Lung; Head and Neck Neoplasms; Solid tumours; Leukemia, Myeloid, Accelerated Phase; Leukemia; Hematologic Neoplasms 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; Osteosarcoma; Sarcoma, Ewing; Colorectal Neoplasms; Peritoneal Neoplasms; Gastrointestinal Stromal Tumors; Bile Duct Neoplasms; Fallopian Tube Neoplasms; Esophageal adenocarcinoma; Adenoma; Thyroid Neoplasms; Lung Neoplasms; Thymoma; Carcinoma, Hepatocellular; Adenocarcinoma; Melanoma; Neoplasm Metastasis; Gastrointestinal Neoplasms; Somatostatinoma; Carcinoma, Islet Cell; Ovarian Neoplasms; Liver Neoplasms; Hemangiosarcoma; Esophageal Neoplasms; Stomach Neoplasms; Carcinoma, Renal Cell; Rectal Neoplasms; Carcinoid Tumor; Insulinoma; Solid tumours; Colonic Neoplasms; Neoplasms; Carcinoma, Ovarian Epithelial; Pancreatic Neoplasms; Small Cell Lung Carcinoma; Glioblastoma; Carcinoma, Transitional Cell; Carcinoma, Adenoid Cystic; Glucagonoma Details
Cabozantinib S-malate XL-184; BMS-907351 Approved Exelixis Inc Cometriq, Cabometyx Japan Carcinoma, Renal Cell Takeda 2012-11-29 Osteosarcoma; Thyroid Neoplasms; Gliosarcoma; Colorectal Neoplasms; Peritoneal Neoplasms; Bile Duct Neoplasms; Hepatic Insufficiency; Astrocytoma; Breast Neoplasms; Sarcoma, Ewing; Lymphoma; Carcinoma, Adenosquamous; Adenocarcinoma, Clear Cell; Sarcoma, Clear Cell; Medullary thyroid cancer (MTC); Cholangiocarcinoma; Prostatic Neoplasms; Neurofibroma, Plexiform; Urethral Neoplasms; Carcinoma, Neuroendocrine; Meningioma; Carcinoma, Non-Small-Cell Lung; Paraganglioma; Melanoma; Carcinoma, Endometrioid; Thyroid Cancer, Papillary; Adenocarcinoma; Neoplasms, Germ Cell and Embryonal; Carcinoma, Hepatocellular; Neuroblastoma; Glioma; Leukemia, Myeloid, Acute; Carcinoma, Squamous Cell; Endometrial Neoplasms; Lung Neoplasms; Sarcoma, Alveolar Soft Part; Uterine Neoplasms; Fallopian Tube Neoplasms; Carcinoid Tumor; Neurofibromatoses; Seminoma; Carcinoma, Transitional Cell; Glioblastoma; Rejection of liver transplantation; Carcinoma, Merkel Cell; Hepatoblastoma; Pain; Pheochromocytoma; Neoplasms; Carcinoma, Renal Cell; B Details
Ripretinib DCC-2618 Approved Deciphera 擎乐, Qinlock United Kingdom Gastrointestinal Stromal Tumors Deciphera Pharmaceuticals Llc 2020-05-15 Mastocytosis, Systemic; Neoplasms; Gastrointestinal Stromal Tumors Details

임상 약품 정보

Name Research Code Research Phase Company Indications Clinical Trials
Gersizangitide AXT-107 AsclepiX Therapeutics Inc Details
Pexmetinib ARRY-614 Array Biopharma Details
QBH-196 QBH-196 Phase 1 Clinical Shenyang Pharmaceutical University Solid tumours; Stomach Neoplasms Details
Rebastinib Tosylate DP-1919; DCC-2036; DP-1919.TO Phase 2 Clinical Deciphera Solid tumours; Leukemia, Myelogenous, Chronic, BCR-ABL Positive Details
CEP-11981 ESK-981; CEP-11981; SSR-106462; BOL-303213X Phase 2 Clinical Sanofi Neoplasms; Prostatic Neoplasms Details
Trebananib AMG-386; 20060439 Phase 2 Clinical Amgen Inc, Takeda Pharmaceutical Co Ltd Fallopian Tube Neoplasms; Breast Neoplasms; Brain Neoplasms; Prostatic Neoplasms; Sarcoma; Peritoneal Neoplasms; Colorectal Neoplasms; Genital Neoplasms, Female; Gliosarcoma; Endometrial Neoplasms; Carcinoma, Adenosquamous; Lung Neoplasms; Uterine Neoplasms; Leukemia, Myeloid, Acute; Leukemia, Monocytic, Acute; Adenocarcinoma; Carcinoma, Non-Small-Cell Lung; Neoplasm Metastasis; Gastrointestinal Neoplasms; Neoplasms; Solid tumours; Leukemia, Myeloid; Leukemia, Erythroblastic, Acute; Carcinoma; Carcinoma, Renal Cell; Rectal Neoplasms; Hemangiosarcoma; Colonic Neoplasms; Ovarian Neoplasms; Kidney Diseases; Leukemia, Myelomonocytic, Acute; Glioblastoma; Sarcoma, Endometrial Stromal; Central Nervous System Neoplasms; Neuroendocrine Tumors; Leukemia, Megakaryoblastic, Acute; Oligodendroglioma Details
Sitravatinib IND-155305; MG-516; MG-91516; MGCD-516 Phase 3 Clinical Mirati Therapeutics Inc Breast Neoplasms; Carcinoma, Hepatocellular; Gastrointestinal Neoplasms; Uterine Cervical Neoplasms; Carcinoma, Non-Small-Cell Lung; Lung Neoplasms; Carcinoma, Squamous Cell; Mouth Neoplasms; Endometrial Neoplasms; Esophageal Squamous Cell Carcinoma; Hepatic Insufficiency; Ureteral Neoplasms; Kidney Neoplasms; Liposarcoma; Lung Diseases; Uveal melanoma; Triple Negative Breast Neoplasms; Carcinoma, Transitional Cell; Neoplasms; Carcinoma; Squamous Cell Carcinoma of Head and Neck; Carcinoma, Renal Cell; Biliary Tract Neoplasms; Solid tumours 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

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