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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 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

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 Details
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
NPS-1034 HOPE-777; KDDF-201111-02 Neopharma Ltd Details
Zanzalintinib XL-092 Phase 3 Clinical Exelixis Inc Solid tumours; Carcinoma, Renal Cell; Squamous Cell Carcinoma of Head and Neck; Carcinoma, Transitional Cell; Neoplasms; Prostatic Neoplasms, Castration-Resistant; Breast Neoplasms; Colorectal Neoplasms; Carcinoma, Hepatocellular; Carcinoma, Non-Small-Cell Lung Details
Sitravatinib MG-91516; MGCD-516; IND-155305; MG-516 Phase 3 Clinical Mirati Therapeutics Inc Breast Neoplasms; Carcinoma, Hepatocellular; Gastrointestinal Neoplasms; Uterine Cervical Neoplasms; Carcinoma, Non-Small-Cell Lung; Lung Neoplasms; Mouth Neoplasms; Endometrial Neoplasms; Carcinoma, Squamous Cell; Esophageal Squamous Cell Carcinoma; Ureteral Neoplasms; Hepatic Insufficiency; Solid tumours; Liposarcoma; Uveal melanoma; Lung Diseases; Carcinoma, Transitional Cell; Triple Negative Breast Neoplasms; Neoplasms; Carcinoma; Squamous Cell Carcinoma of Head and Neck; Carcinoma, Renal Cell; Biliary Tract Neoplasms; Kidney Neoplasms Details
Q-702 Q-702 Phase 2 Clinical Vichem Chemie, Max Planck Institute of Biochemistry, Lead Discovery Center GmbH Solid tumours; Liver Neoplasms; Esophageal Neoplasms; Stomach Neoplasms; Neoplasms; Neoplasm Metastasis; Uterine Cervical 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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