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MERTK

Brief Information

Name:Tyrosine-protein kinase Mer
Target Synonym:EC 2.7.10,MER,MERTK,C-Mer Proto-Oncogene Tyrosine Kinase,Receptor Tyrosine Kinase MerTK,Tyrosine-Protein Kinase Mer,EC 2.7.10.1,STK Kinase,EC:2.7.10.1,Proto-oncogene c-Mer,MER Proto-Oncogene, Tyrosine Kinase,MER Receptor Tyrosine Kinase,Tyro12,C-Eyk,C-Mer,RP38,c-Mer Tyrosine Kinase
Number of Launched Drugs:1
Number of Drugs in Clinical Trials:6
Lastest Research Phase:Approved

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Part of Bioactivity data

MEK-H52H6-SPR
 MERTK SPR

Human MERTK, His Tag (Cat. No. MEK-H52H6) immobilized on CM5 Chip can bind Human GAS6, His Tag (Cat. No. GA6-H5249) with an affinity constant of 50.9 nM as determined in SPR assay (Biacore 8K) (Routinely tested).

MEK-M52H9-MALS-HPLC
MERTK MALS images

The purity of Mouse MERTK, His Tag (Cat. No. MEK-M52H9) is more than 90% and the molecular weight of this protein is around 70-95 kDa verified by SEC-MALS.

Synonym Name

MERTK,Mer

Background

Tyrosine-protein kinase Mer(MERTK) is a member of the TYRO3/AXL/MER (TAM) receptor kinase family and encodes a transmembrane protein with two fibronectin type-III domains, two Ig-like C2-type (immunoglobulin-like) domains, and one tyrosine kinase domain. Following activation by ligand, interacts with GRB2 or PLCG2 and induces phosphorylation of MAPK1, MAPK2, FAK/PTK2 or RAC1. MERTK signaling plays a role in various processes such as macrophage clearance of apoptotic cells, platelet aggregation, cytoskeleton reorganization and engulfment. Functions in the retinal pigment epithelium (RPE) as a regulator of rod outer segments fragments phagocytosis. Plays also an important role in inhibition of Toll-like receptors (TLRs)-mediated innate immune response by activating STAT1, which selectively induces production of suppressors of cytokine signaling SOCS1 and SOCS3.

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 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

Clinical Drug Information

Name Research Code Research Phase Company Indications Clinical Trials
INCB-081776 INCB-81776; INCB-081776 Phase 1 Clinical Incyte Corp Solid tumours; Neoplasms Details
MRX-2843 MRX-2843; UNC-2025; UNC-2371 Phase 2 Clinical Meryx Inc, University Of North Carolina At Chapel Hill, University Of Colorado At Denver Leukemia; Solid tumours; Neoplasms; Pathologic Processes; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Leukemia, Myeloid, Acute; Lung Neoplasms; Neoplastic Processes; Carcinoma, Non-Small-Cell Lung; Neoplasm Metastasis Details

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