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Axl

概要

Name:AXL receptor tyrosine kinase
Target Synonym:EC:2.7.10.1,EC 2.7.10,UFO,AXL Transforming Sequence/Gene,AXL Oncogene,EC 2.7.10.1,JTK11,Tyro7,ARK,Tyrosine-protein kinase receptor UFO,AXL,AXL Receptor Tyrosine Kinase
Number of Launched Drugs:2
Number of Drugs in Clinical Trials:28
Lastest Research Phase:Approved

ライセンス

Project Name Modality Therapeutic Area Indications Stage Right Available
AXL inhibitor Small molecule Oncology/Cancer STK11_mut NSCLC,other cancers Phase I Global

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製造番号 種類 製品説明 構造 純度 特徴
AXL-H82F9 Human Biotinylated Human AXL Protein, Fc,Avitag™ (MALS verified)
AXL-H82F9-structure
AXL-H82F9-sds
AXL-H5253 Human Human Axl Protein, Fc Tag (MALS verified)
AXL-H5253-structure
AXL-H5253-sds
AXL-C52H3 Cynomolgus Cynomolgus Axl Protein, His Tag
AXL-C52H3-structure
AXL-C52H3-sds
AXL-H5226 Human Human Axl Protein, His Tag (SPR verified)
AXL-H5226-structure
AXL-H5226-sds
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生物活性データの一部

AXL-H5253-SPR
Axl SPR

Human Axl, Fc Tag (Cat. No. AXL-H5253) captured on CM5 chip via Anti-human IgG Fc antibodies surface can bind Human GAS6, His Tag (Cat. No. GA6-H5249) with an affinity constant of 1.23 nM as determined in a SPR assay (Biacore 8K) (Routinely tested).

Protocol
AXL-H5226-SPR
Axl SPR

Human Axl, His Tag (Cat. No. AXL-H5226) immobilized on CM5 Chip can bind Human GAS6, His Tag (Cat. No. GA6-H5249) with an affinity constant of 3.4 nM as determined in SPR assay (Biacore 8K) (QC tested).

Protocol

Synonym Name

AXL,UFO

Background

AXL Receptor Tyrosine Kinase is also known as Tyrosine-protein kinase receptor UFO, which belongs to the protein kinase superfamily, Tyr protein kinase family and AXL/UFO subfamily. AXL contains two fibronectin type-III domains, two Ig-like C2-type (immunoglobulin-like) domains and one protein kinase domain. AXL is highly expressed in metastatic colon tumors. AXL is activated by GAS6-binding and subsequent autophosphorylation. AXL is involved in signal transduction from the extracellular matrix into the cytoplasm by binding growth factors, and thus implicated in the stimulation of cell proliferation.

Clinical and Translational Updates

公開薬物情報

Name Research Code Research Phase Company First Brand Name First Approved Country First Indication First Approved Company First Approved Date Indications Clinical Trials
Gilteritinib Fumarate ASP-2215 hemifumarate; ASP-2215; 66D-92MGC8M (UNII code) Approved Astellas Pharma Inc Xospata Japan Leukemia, Myeloid, Acute Astellas Pharma Inc 2018-09-21 Solid tumours; Renal Insufficiency; Hepatic Insufficiency; Lung Neoplasms; Leukemia, Myeloid, Acute; Carcinoma, Non-Small-Cell Lung Details
Cabozantinib S-malate XL-184; BMS-907351 Approved Exelixis Inc Cometriq, Cabometyx United States Carcinoma, Neuroendocrine; Thyroid Neoplasms Exelixis Inc 2012-11-29 Urethral Neoplasms; Leukemia, Myeloid, Acute; Thyroid Neoplasms; Gliosarcoma; Colorectal Neoplasms; Astrocytoma; Hepatic Insufficiency; Peritoneal Neoplasms; Bile Duct Neoplasms; Sarcoma, Clear Cell; Uterine Neoplasms; Adenocarcinoma, Clear Cell; Sarcoma, Ewing; Carcinoma, Adenosquamous; Breast Neoplasms; Neurofibroma, Plexiform; Osteosarcoma; Prostatic Neoplasms; Sarcoma; Medullary thyroid cancer (MTC); Carcinoma, Hepatocellular; Melanoma; Paraganglioma; Meningioma; Neoplasms, Germ Cell and Embryonal; Neoplasm Metastasis; Carcinoma, Non-Small-Cell Lung; Adenocarcinoma; Carcinoma, Endometrioid; Thyroid Cancer, Papillary; Brain Neoplasms; Carcinoma, Neuroendocrine; Sarcoma, Alveolar Soft Part; Lymphoma; Fallopian Tube Neoplasms; Brain metastases; Glioma; Endometrial Neoplasms; Carcinoma, Squamous Cell; Carcinoid Tumor; Glioblastoma; Skin Neoplasms; Neoplasms; Carcinoma, Papillary; Hepatoblastoma; Pheochromocytoma; Pain; Rejection of liver transplantation; Carcinoma, Renal Cell; Pancreatic neuroendocrine tumors Details
Gilteritinib Fumarate ASP-2215 hemifumarate; ASP-2215; 66D-92MGC8M (UNII code) Approved Astellas Pharma Inc Xospata Japan Leukemia, Myeloid, Acute Astellas Pharma Inc 2018-09-21 Solid tumours; Renal Insufficiency; Hepatic Insufficiency; Lung Neoplasms; Leukemia, Myeloid, Acute; Carcinoma, Non-Small-Cell Lung Details
Cabozantinib S-malate XL-184; BMS-907351 Approved Exelixis Inc Cometriq, Cabometyx United States Carcinoma, Neuroendocrine; Thyroid Neoplasms Exelixis Inc 2012-11-29 Urethral Neoplasms; Leukemia, Myeloid, Acute; Thyroid Neoplasms; Gliosarcoma; Colorectal Neoplasms; Astrocytoma; Hepatic Insufficiency; Peritoneal Neoplasms; Bile Duct Neoplasms; Sarcoma, Clear Cell; Uterine Neoplasms; Adenocarcinoma, Clear Cell; Sarcoma, Ewing; Carcinoma, Adenosquamous; Breast Neoplasms; Neurofibroma, Plexiform; Osteosarcoma; Prostatic Neoplasms; Sarcoma; Medullary thyroid cancer (MTC); Carcinoma, Hepatocellular; Melanoma; Paraganglioma; Meningioma; Neoplasms, Germ Cell and Embryonal; Neoplasm Metastasis; Carcinoma, Non-Small-Cell Lung; Adenocarcinoma; Carcinoma, Endometrioid; Thyroid Cancer, Papillary; Brain Neoplasms; Carcinoma, Neuroendocrine; Sarcoma, Alveolar Soft Part; Lymphoma; Fallopian Tube Neoplasms; Brain metastases; Glioma; Endometrial Neoplasms; Carcinoma, Squamous Cell; Carcinoid Tumor; Glioblastoma; Skin Neoplasms; Neoplasms; Carcinoma, Papillary; Hepatoblastoma; Pheochromocytoma; Pain; Rejection of liver transplantation; Carcinoma, Renal Cell; Pancreatic neuroendocrine tumors Details

臨床試験情報

Name Research Code Research Phase Company Indications Clinical Trials
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, Non-Small-Cell Lung; Carcinoma, Hepatocellular Details
KC1036 KC1036; KC-1036 Phase 3 Clinical Beijing Konruns Pharmaceutical Co Ltd Hematologic Neoplasms; Solid tumours; Digestive System Neoplasms; Sarcoma, Ewing; Thymus Neoplasms; Esophageal Squamous Cell Carcinoma; Adenocarcinoma; Neoplasm Metastasis 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; Metastatic breast cancer; Mouth Neoplasms; Endometrial Neoplasms; Carcinoma, Squamous Cell; Esophageal Squamous Cell Carcinoma; Lung Neoplasms; Ureteral Neoplasms; Hepatic Insufficiency; Solid tumours; Liposarcoma; Uveal melanoma; Lung Diseases; Carcinoma, Transitional Cell; Neoplasms; Triple Negative Breast Neoplasms; Carcinoma; Squamous Cell Carcinoma of Head and Neck; Carcinoma, Renal Cell; Biliary Tract Neoplasms; Kidney Neoplasms Details
Ningetinib Tosylate CT-053-PTSA; CT-053 Phase 2 Clinical Hec Pharm Co Ltd Intestinal Neoplasms; Solid tumours; Carcinoma, Renal Cell; Stomach Neoplasms; Leukemia, Myeloid, Acute; Lung Neoplasms; Carcinoma, Non-Small-Cell Lung Details
Mecbotamab vedotin BA-3011; BA3011; BA 3011 Phase 2 Clinical Bioatla Ovarian Neoplasms; Sarcoma, Synovial; Liposarcoma; Osteosarcoma; Sarcoma, Ewing; Sarcoma; Carcinoma, Non-Small-Cell Lung 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; Lymphoma, Mantle-Cell; Breast Neoplasms; Cholangiocarcinoma; Colorectal Neoplasms; Leukemia, Myeloid, Acute; Lymphoma, Non-Hodgkin; Gallbladder Neoplasms; Neoplasm Metastasis; Carcinoma, Non-Small-Cell Lung Details
ONO-7475 ONO-7475 Phase 2 Clinical Ono Pharmaceutical Co Ltd Leukemia; Solid tumours; Myelodysplastic Syndromes; Leukemia, Myeloid, Acute Details
Bemcentinib BGB-324; R-428 Phase 2 Clinical Rigel Pharmaceuticals Inc Adenocarcinoma of Lung; Myelodysplastic Syndromes; Pancreatic Neoplasms; Inflammatory Breast Neoplasms; Triple Negative Breast Neoplasms; Coronavirus Disease 2019 (COVID-19); Mesothelioma; Lung Neoplasms; Leukemia, Myeloid, Acute; 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
Enapotamab vedotin AXL-107-MMAE Phase 2 Clinical Genmab A/S Ovarian Neoplasms; Solid tumours; Neoplasms; Sarcoma; Thyroid Neoplasms; Endometrial Neoplasms; Carcinoma, Non-Small-Cell Lung; Melanoma; Uterine Cervical Neoplasms Details
CCT301-38 CCT301-38; CCT301-38 AXL Phase 2 Clinical F1 Oncology, Bioatla Carcinoma, Renal Cell; Rhinitis, Allergic, Seasonal Details
XZB-0004 XZB-0004; SLC-0211; SLC-391 Phase 2 Clinical Xuanzhu (Shijiazhuang) Biotechnology Co Ltd Solid tumours; Hematologic Neoplasms; Myelodysplastic Syndromes; Leukemia, Myeloid, Acute; Lung Neoplasms; Carcinoma, Non-Small-Cell Lung; Foodborne Diseases Details
Butylidenephthalide BDPH; HK-001; NSC-325307; LF-001 (Everfront Biotech) Phase 2 Clinical Everfront Biotech Co Ltd Glioma; Amyotrophic Lateral Sclerosis 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
Dubermatinib TP-0903 Phase 1 Clinical Sumitomo Dainippon Ovarian Neoplasms; Solid tumours; Colorectal Neoplasms; Leukemia, Myeloid, Acute; Leukemia, Lymphocytic, Chronic, B-Cell; Melanoma; Carcinoma, Non-Small-Cell Lung Details
INCB-081776 INCB-81776; INCB-081776 Phase 1 Clinical Incyte Corp Solid tumours; Squamous Cell Carcinoma of Head and Neck Details
BPI-9016 BPI-9016; BPI-9016M Phase 1 Clinical Betta Pharmaceuticals Co Ltd Solid tumours; Carcinoma, Non-Small-Cell Lung Details
Mipasetamab uzoptirine ADCT-601; BGB-601 Phase 1 Clinical Adc Therapeutics Sa Solid tumours Details
NTQ-2494 NTQ2494; NTQ-2494 Phase 1 Clinical Nanjing Zhengda Tianqing Pharmaceutical Co Ltd Solid tumours; Hematologic Neoplasms; Leukemia, Myeloid, Acute Details
AB-801 AB-801 Phase 1 Clinical Arcus Biosciences Inc Neoplasms Details
FC-084-CSA FC084CSA; FC-084-CSA Phase 1 Clinical FindCure Biosciences (ZhongShan) Co Ltd Solid tumours Details
NP-107 NP107; NP-107 Phase 1 Clinical Shanghai Nawei Biotechnology Co Ltd Solid tumours Details
TT-00973 TT-00973 Phase 1 Clinical TransThera Sciences (Nanjing) Inc Solid tumours Details
AGX-0073 AGX-0073 Phase 1 Clinical Shanghai Aojian Biological Technology Co Ltd Solid tumours Details
PF-07265807 PF-07265807 Phase 1 Clinical Pfizer Inc Solid tumours; Neoplasm Metastasis Details
NP-01 (Shijiazhuang No.4 Pharmaceutical/Nanjing Nadingfei Medical Technology) NP-01 Phase 1 Clinical Shijiazhuang No 4 Pharmaceutical Co Ltd, Nanjing Nadingfei Pharmaceutical Technology Co Ltd Solid tumours; Liver Neoplasms; Stomach Neoplasms; Lung Neoplasms Details
cancer therapeutics (BerGenBio) BGB-101; BGB-109; BGB-003; BGB-001 Phase 1 Clinical Bergenbio 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, Non-Small-Cell Lung; Carcinoma, Hepatocellular Details
KC1036 KC1036; KC-1036 Phase 3 Clinical Beijing Konruns Pharmaceutical Co Ltd Hematologic Neoplasms; Solid tumours; Digestive System Neoplasms; Sarcoma, Ewing; Thymus Neoplasms; Esophageal Squamous Cell Carcinoma; Adenocarcinoma; Neoplasm Metastasis 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; Metastatic breast cancer; Mouth Neoplasms; Endometrial Neoplasms; Carcinoma, Squamous Cell; Esophageal Squamous Cell Carcinoma; Lung Neoplasms; Ureteral Neoplasms; Hepatic Insufficiency; Solid tumours; Liposarcoma; Uveal melanoma; Lung Diseases; Carcinoma, Transitional Cell; Neoplasms; Triple Negative Breast Neoplasms; Carcinoma; Squamous Cell Carcinoma of Head and Neck; Carcinoma, Renal Cell; Biliary Tract Neoplasms; Kidney Neoplasms Details
Ningetinib Tosylate CT-053-PTSA; CT-053 Phase 2 Clinical Hec Pharm Co Ltd Intestinal Neoplasms; Solid tumours; Carcinoma, Renal Cell; Stomach Neoplasms; Leukemia, Myeloid, Acute; Lung Neoplasms; Carcinoma, Non-Small-Cell Lung Details
Mecbotamab vedotin BA-3011; BA3011; BA 3011 Phase 2 Clinical Bioatla Ovarian Neoplasms; Sarcoma, Synovial; Liposarcoma; Osteosarcoma; Sarcoma, Ewing; Sarcoma; Carcinoma, Non-Small-Cell Lung 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; Lymphoma, Mantle-Cell; Breast Neoplasms; Cholangiocarcinoma; Colorectal Neoplasms; Leukemia, Myeloid, Acute; Lymphoma, Non-Hodgkin; Gallbladder Neoplasms; Neoplasm Metastasis; Carcinoma, Non-Small-Cell Lung Details
ONO-7475 ONO-7475 Phase 2 Clinical Ono Pharmaceutical Co Ltd Leukemia; Solid tumours; Myelodysplastic Syndromes; Leukemia, Myeloid, Acute Details
Bemcentinib BGB-324; R-428 Phase 2 Clinical Rigel Pharmaceuticals Inc Adenocarcinoma of Lung; Myelodysplastic Syndromes; Pancreatic Neoplasms; Inflammatory Breast Neoplasms; Triple Negative Breast Neoplasms; Coronavirus Disease 2019 (COVID-19); Mesothelioma; Lung Neoplasms; Leukemia, Myeloid, Acute; 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
Enapotamab vedotin AXL-107-MMAE Phase 2 Clinical Genmab A/S Ovarian Neoplasms; Solid tumours; Neoplasms; Sarcoma; Thyroid Neoplasms; Endometrial Neoplasms; Carcinoma, Non-Small-Cell Lung; Melanoma; Uterine Cervical Neoplasms Details
CCT301-38 CCT301-38; CCT301-38 AXL Phase 2 Clinical F1 Oncology, Bioatla Carcinoma, Renal Cell; Rhinitis, Allergic, Seasonal Details
XZB-0004 XZB-0004; SLC-0211; SLC-391 Phase 2 Clinical Xuanzhu (Shijiazhuang) Biotechnology Co Ltd Solid tumours; Hematologic Neoplasms; Myelodysplastic Syndromes; Leukemia, Myeloid, Acute; Lung Neoplasms; Carcinoma, Non-Small-Cell Lung; Foodborne Diseases Details
Butylidenephthalide BDPH; HK-001; NSC-325307; LF-001 (Everfront Biotech) Phase 2 Clinical Everfront Biotech Co Ltd Glioma; Amyotrophic Lateral Sclerosis 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
Dubermatinib TP-0903 Phase 1 Clinical Sumitomo Dainippon Ovarian Neoplasms; Solid tumours; Colorectal Neoplasms; Leukemia, Myeloid, Acute; Leukemia, Lymphocytic, Chronic, B-Cell; Melanoma; Carcinoma, Non-Small-Cell Lung Details
INCB-081776 INCB-81776; INCB-081776 Phase 1 Clinical Incyte Corp Solid tumours; Squamous Cell Carcinoma of Head and Neck Details
BPI-9016 BPI-9016; BPI-9016M Phase 1 Clinical Betta Pharmaceuticals Co Ltd Solid tumours; Carcinoma, Non-Small-Cell Lung Details
Mipasetamab uzoptirine ADCT-601; BGB-601 Phase 1 Clinical Adc Therapeutics Sa Solid tumours Details
NTQ-2494 NTQ2494; NTQ-2494 Phase 1 Clinical Nanjing Zhengda Tianqing Pharmaceutical Co Ltd Solid tumours; Hematologic Neoplasms; Leukemia, Myeloid, Acute Details
AB-801 AB-801 Phase 1 Clinical Arcus Biosciences Inc Neoplasms Details
FC-084-CSA FC084CSA; FC-084-CSA Phase 1 Clinical FindCure Biosciences (ZhongShan) Co Ltd Solid tumours Details
NP-107 NP107; NP-107 Phase 1 Clinical Shanghai Nawei Biotechnology Co Ltd Solid tumours Details
TT-00973 TT-00973 Phase 1 Clinical TransThera Sciences (Nanjing) Inc Solid tumours Details
AGX-0073 AGX-0073 Phase 1 Clinical Shanghai Aojian Biological Technology Co Ltd Solid tumours Details
PF-07265807 PF-07265807 Phase 1 Clinical Pfizer Inc Solid tumours; Neoplasm Metastasis Details
NP-01 (Shijiazhuang No.4 Pharmaceutical/Nanjing Nadingfei Medical Technology) NP-01 Phase 1 Clinical Shijiazhuang No 4 Pharmaceutical Co Ltd, Nanjing Nadingfei Pharmaceutical Technology Co Ltd Solid tumours; Liver Neoplasms; Stomach Neoplasms; Lung Neoplasms Details
cancer therapeutics (BerGenBio) BGB-101; BGB-109; BGB-003; BGB-001 Phase 1 Clinical Bergenbio Details
NPS-1034 HOPE-777; KDDF-201111-02 Neopharma Ltd Details

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