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FAP

概要

Name:Prolyl endopeptidase FAP
Target Synonym:Post-Proline Cleaving Enzyme,FAPalpha,SIMP,Fibroblast Activation Protein, Alpha,Serine Integral Membrane Protease,Prolyl Endopeptidase FAP,EC 3.4.21.26,EC 3.4.14.5,EC 3.4.21.-,DPPIV,FAPA,170 kDa melanoma membrane-bound gelatinase,Seprase,Gelatine degradation protease FAP,Dipeptidyl peptidase FAP,Fibroblast activation protein alpha,APCE,Integral membrane serine protease,Surface-expressed protease,FAP
Number of Launched Drugs:0
Number of Drugs in Clinical Trials:26
Lastest Research Phase:Phase 2 Clinical

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製造番号 種類 製品説明 構造 純度 特徴
CHEK-ATP184 Human HEK293/Human FAP Stable Cell Line
MBS-K077 Human Human FAP-coupled Magnetic Beads
FAP-M82Q8 Mouse Biotinylated Mouse FAP Protein, His,Avitag™, active dimer (MALS verified)
FAP-M82Q8-structure
FAP-M82Q8-sds
FAP-R5246 Rat Rat FAP Protein, His Tag, active dimer (MALS verified)
FAP-R5246-structure
FAP-R5246-sds
FAP-HP245 Human PE-Labeled Human FAP Protein, His Tag (Site-specific conjugation)
FAP-HP245-structure
FAP-C52H3 Cynomolgus Cynomolgus FAP Protein, His Tag, active dimer (MALS verified)
FAP-C52H3-structure
FAP-C52H3-sds
FAP-M52H3 Mouse Mouse FAP Protein, His Tag, active dimer (MALS verified)
FAP-M52H3-structure
FAP-M52H3-sds
FAP-C82Q5 Cynomolgus Biotinylated Cynomolgus FAP Protein, His,Avitag™, active dimer (MALS verified)
FAP-C82Q5-structure
FAP-C82Q5-sds
FAP-HF263 Human FITC-Labeled Human FAP Protein, Fc Tag
FAP-HF263-structure
FAP-HF263-sds
FAP-H82Q6 Human Biotinylated Human FAP Protein, His,Avitag™, active dimer (MALS verified)
FAP-H82Q6-structure
FAP-H82Q6-sds
FAP-HF243 Human FITC-Labeled Human FAP Protein, His Tag
FAP-HF243-structure
FAP-HF243-sds
FAP-H5244 Human Human FAP Protein, His Tag, active dimer (MALS verified)
FAP-H5244-structure
FAP-H5244-sds
FAP-H5263 Human Human FAP Protein, Fc Tag, active dimer (MALS verified)
FAP-H5263-structure
FAP-H5263-sds
ACRO Quality

生物活性データの一部

CHEK-ATP184-Cell-based assay
FAP FACS

Expression analysis of human FAP on HEK293/Human FAP Stable Cell Line by FACS.
Cell surface staining was performed on HEK293/Human FAP Stable Cell Line or negative control cell using anti-human FAP antibody followed by staining with PE anti-human IgG Fc Antibody.

Protocol
FAP-HP245-Cell-based assay
FACS assay shows that recombinant Biotinylated FACS

5e5 of anti-FAP CAR-293 cells were stained with 100 μL of 1:25 dilution (4 μL stock solution in 100 μL FACS buffer) of PE-Labeled Human FAP, His Tag (Cat. No. FAP-HP245) and negative control protein respectively. PE signal was used to evaluate the binding activity (QC tested).

Protocol
FAP-R5246-SPR
FAP SPR

Anti-FAP Antibody, Mouse IgG2a (FAP5) captured on CM5 chip via anti-mouse antibodies surface can bind Rat FAP, His Tag (Cat. No. FAP-R5246) with an affinity constant of 0.839 nM as determined in a SPR assay (Biacore 8K) (Routinely tested).

Protocol
FAP-C52H3-SPR
FAP SPR

Anti-FAP Antibody, Mouse IgG2a (FAP5) captured on CM5 chip via anti-mouse antibodies surface can bind Cynomolgus FAP, His Tag (Cat. No. FAP-C52H3) with an affinity constant of 3.10 nM as determined in a SPR assay (Biacore 8K) (Routinely tested).

Protocol

Synonym Name

FAP,FAPalpha,SIMP,Seprase,APCE

Background

FAP (also known as seprase) is a Type II transmembrane serine protease. Both plasma membrane and soluble forms exhibit post-proline cleaving endopeptidase activity, with a marked preference for Ala/Ser-Gly-Pro-Ser/Asn/Ala consensus sequences. Degrade also gelatin, heat-denatured type I collagen. Also has dipeptidyl peptidase activity, with a preference for Ala-Pro, Ile-Pro, Gly-Pro, Arg-Pro and Pro-Pro. The plasma membrane form, in association with either DPP4, PLAUR or integrins, is involved in the pericellular proteolysis of the extracellular matrix (ECM), and hence promotes cell adhesion, migration and invasion through the ECM. Promotes glioma cell invasion through the brain parenchyma by degrading the proteoglycan brevican. Acts as a tumor suppressor in melanocytic cells through regulation of cell proliferation and survival in a serine protease activity-independent manner.

Clinical and Translational Updates

臨床試験情報

Name Research Code Research Phase Company Indications Clinical Trials
Talabostat PT-100; BXCL-701 Phase 2 Clinical Point Therapeutics Neuroblastoma; Adenocarcinoma; Melanoma; Carcinoma, Non-Small-Cell Lung; Neoplasm Metastasis; Leukemia, Lymphocytic, Chronic, B-Cell; Neoplasms, Germ Cell and Embryonal; Carcinoma, Small Cell; Carcinoma, Pancreatic Ductal; Lung Neoplasms; Leukemia, Myeloid, Acute; Prostatic Neoplasms; Liver Neoplasms; Brain Neoplasms; Sarcoma; Neuroendocrine Tumors; Central Nervous System Neoplasms; Small Cell Lung Carcinoma; Pancreatic Neoplasms; Skin Neoplasms; Myelodysplastic Syndromes; Kidney Neoplasms; Solid tumours; Ovarian Neoplasms Details
[18F]FAPI-74 FAPI-74; [18F]FAPI-74 Phase 2 Clinical Sofie Biliary Tract Neoplasms; Stomach Neoplasms; Pancreatic Neoplasms; Cholangiocarcinoma; Colorectal Neoplasms; Carcinoma, Pancreatic Ductal; Carcinoma, Hepatocellular; Gastrointestinal Neoplasms Details
68Ga-FAP-2286 68Ga-FAP-2286; 68-Ga-FAP-2286 Phase 2 Clinical 3B Pharmaceuticals GmbH Solid tumours; Neoplasm Metastasis Details
68Ga-FAPI-46 [68Ga]FAPI-46; 68Ga-FAPI-46 Phase 2 Clinical Karolinska University Hospital Pancreatic Neoplasms; Alveolitis, Extrinsic Allergic; Pneumoconiosis; Carcinoma, Pancreatic Ductal; Bile Duct Neoplasms; Lung Diseases, Interstitial; Pulmonary Fibrosis; Neoplasms; Carcinoma, Ovarian Epithelial; Adenomatous Polyposis Coli; Pneumonia; Esophageal Neoplasms; Metabolic Dysfunction-Associated Steatotic Liver Disease; Idiopathic Interstitial Pneumonias; Radiation Pneumonitis; Stomach Neoplasms; Ovarian Neoplasms Details
RO-7122290 RO-7122290; RG-7827 Phase 2 Clinical F. Hoffmann-La Roche Ltd Colorectal Neoplasms Details
NG-641 EnAd-FAP-BiTE; EnAd-FAP-Tac; NG-641; NG-aFAP Phase 1 Clinical Akamis Bio Ltd, University Of Oxford Squamous Cell Carcinoma of Head and Neck; Neoplasms, Glandular and Epithelial; Neoplasm Metastasis Details
Simlukafusp alfa FAP-IL2v; RG-7461; aFAP-IL2v; RO-6874281; FAP-IL2v FP Phase 1 Clinical F. Hoffmann-La Roche Ltd Head and Neck Neoplasms; Solid tumours; Carcinoma, Renal Cell; Esophageal Neoplasms; Breast Neoplasms; Uterine Cervical Neoplasms; Melanoma Details
Nectin4/FAP-targeted CAR-T cell therapy (The Sixth Affiliated Hospital of Wenzhou Medical University) Phase 1 Clinical Wenzhou Medical University, The Sixth Affiliated Hospital Of Wenzhou Medical University Solid tumours Details
OMTX-705 OMTX-705 Phase 1 Clinical Oncomatryx Biopharma Sl Solid tumours Details
MP-0310 MP-0310; AMG-506 Phase 1 Clinical Molecular Partners Ag, Amgen Inc Solid tumours Details
68 Ga-OncoFAP-DOTAGA 68 Ga-OncoFAP Phase 1 Clinical Blue Earth Diagnostics, Philochem Solid tumours Details
AAA-614 AAA-614; FAP-2286 Phase 1 Clinical Novartis Ag Solid tumours Details
18F-AlF-FAPi-04 18F-AlF-FAPi-04 Phase 1 Clinical Affiliated Hospital Of North Sichuan Medical College Solid tumours Details
177Lu-EB-FAPI(Peking Union Medical College Hospital) 177Lu-EB-FAPI(Peking Union Medical College Hospital) Phase 1 Clinical Peking Union Medical College Hospital Neoplasm Metastasis Details
68Ga-FAPI(Peking Union Medical College Hospital) 68Ga-FAPI(Peking Union Medical College Hospital) Phase 1 Clinical Peking Union Medical College Hospital Neoplasm Metastasis Details
177Lu-EB-FAPI 177Lu-EB-FAPI Phase 1 Clinical Zhejiang University Pancreatic Neoplasms; Cholangiocarcinoma Details
RTX-1363-S RTX-1363S; RTX-1363-S Phase 1 Clinical Ratio Therapeutics Inc Stomach Neoplasms; Pancreatic Neoplasms; Breast Neoplasms; Lung Neoplasms Details
177Lu-DOTA-EB-FAPI Phase 1 Clinical The First Affiliated Hospital Of Xiamen University Solid tumours; Adenocarcinoma, Follicular; Thyroid Neoplasms; Thyroid Cancer, Papillary Details
68Ga/64Cu-FAPI-XT117 68Ga/64Cu-FAPI-XT117 Phase 1 Clinical Pla General Hospital Solid tumours Details
177Lu-LNC1004 177Lu-LNC1004; 177Lu-LNC-1004 Phase 1 Clinical Shanghai Lannacheng Biotechnology Co Ltd Solid tumours Details
68Ga-FAPI-RGD 68Ga-FAPI-RGD Phase 1 Clinical Peking Union Medical College Hospital Lung Neoplasms Details
SHR-7367 SHR7367; SHR-7367 Phase 1 Clinical Shanghai Hengrui Pharmaceutical Co Ltd Solid tumours; Neoplasms Details
177Lu-PNT6555(Point Biopharma) PNT-6555 Phase 1 Clinical Solid tumours; Squamous Cell Carcinoma of Head and Neck; Esophageal Neoplasms; Sarcoma; Cholangiocarcinoma; Colorectal Neoplasms; Carcinoma, Pancreatic Ductal; Melanoma Details
RO-7300490 RO-7300490; RG-6189 Phase 1 Clinical F. Hoffmann-La Roche Ltd Solid tumours; Neoplasms Details
[90Y] YFAPI-46 Clinical German Cancer Consortium (Dktk), University of Duisburg-Essen Solid tumours Details
3BP-3940 3BP-3940 Clinical Johannes Gutenberg University Of Mainz, 3B Pharmaceuticals GmbH Neoplasms Details
64Cu-LNTH-1363S 64Cu-LNTH-1363S Details
177Lu-FAP-2286 177Lu-FAP-2286 3B Pharmaceuticals GmbH Solid tumours Details
Talabostat PT-100; BXCL-701 Phase 2 Clinical Point Therapeutics Neuroblastoma; Adenocarcinoma; Melanoma; Carcinoma, Non-Small-Cell Lung; Neoplasm Metastasis; Leukemia, Lymphocytic, Chronic, B-Cell; Neoplasms, Germ Cell and Embryonal; Carcinoma, Small Cell; Carcinoma, Pancreatic Ductal; Lung Neoplasms; Leukemia, Myeloid, Acute; Prostatic Neoplasms; Liver Neoplasms; Brain Neoplasms; Sarcoma; Neuroendocrine Tumors; Central Nervous System Neoplasms; Small Cell Lung Carcinoma; Pancreatic Neoplasms; Skin Neoplasms; Myelodysplastic Syndromes; Kidney Neoplasms; Solid tumours; Ovarian Neoplasms Details
[18F]FAPI-74 FAPI-74; [18F]FAPI-74 Phase 2 Clinical Sofie Biliary Tract Neoplasms; Stomach Neoplasms; Pancreatic Neoplasms; Cholangiocarcinoma; Colorectal Neoplasms; Carcinoma, Pancreatic Ductal; Carcinoma, Hepatocellular; Gastrointestinal Neoplasms Details
68Ga-FAP-2286 68Ga-FAP-2286; 68-Ga-FAP-2286 Phase 2 Clinical 3B Pharmaceuticals GmbH Solid tumours; Neoplasm Metastasis Details
68Ga-FAPI-46 [68Ga]FAPI-46; 68Ga-FAPI-46 Phase 2 Clinical Karolinska University Hospital Pancreatic Neoplasms; Alveolitis, Extrinsic Allergic; Pneumoconiosis; Carcinoma, Pancreatic Ductal; Bile Duct Neoplasms; Lung Diseases, Interstitial; Pulmonary Fibrosis; Neoplasms; Carcinoma, Ovarian Epithelial; Adenomatous Polyposis Coli; Pneumonia; Esophageal Neoplasms; Metabolic Dysfunction-Associated Steatotic Liver Disease; Idiopathic Interstitial Pneumonias; Radiation Pneumonitis; Stomach Neoplasms; Ovarian Neoplasms Details
RO-7122290 RO-7122290; RG-7827 Phase 2 Clinical F. Hoffmann-La Roche Ltd Colorectal Neoplasms Details
NG-641 EnAd-FAP-BiTE; EnAd-FAP-Tac; NG-641; NG-aFAP Phase 1 Clinical Akamis Bio Ltd, University Of Oxford Squamous Cell Carcinoma of Head and Neck; Neoplasms, Glandular and Epithelial; Neoplasm Metastasis Details
Simlukafusp alfa FAP-IL2v; RG-7461; aFAP-IL2v; RO-6874281; FAP-IL2v FP Phase 1 Clinical F. Hoffmann-La Roche Ltd Head and Neck Neoplasms; Solid tumours; Carcinoma, Renal Cell; Esophageal Neoplasms; Breast Neoplasms; Uterine Cervical Neoplasms; Melanoma Details
Nectin4/FAP-targeted CAR-T cell therapy (The Sixth Affiliated Hospital of Wenzhou Medical University) Phase 1 Clinical Wenzhou Medical University, The Sixth Affiliated Hospital Of Wenzhou Medical University Solid tumours Details
OMTX-705 OMTX-705 Phase 1 Clinical Oncomatryx Biopharma Sl Solid tumours Details
MP-0310 MP-0310; AMG-506 Phase 1 Clinical Molecular Partners Ag, Amgen Inc Solid tumours Details
68 Ga-OncoFAP-DOTAGA 68 Ga-OncoFAP Phase 1 Clinical Blue Earth Diagnostics, Philochem Solid tumours Details
AAA-614 AAA-614; FAP-2286 Phase 1 Clinical Novartis Ag Solid tumours Details
18F-AlF-FAPi-04 18F-AlF-FAPi-04 Phase 1 Clinical Affiliated Hospital Of North Sichuan Medical College Solid tumours Details
177Lu-EB-FAPI(Peking Union Medical College Hospital) 177Lu-EB-FAPI(Peking Union Medical College Hospital) Phase 1 Clinical Peking Union Medical College Hospital Neoplasm Metastasis Details
68Ga-FAPI(Peking Union Medical College Hospital) 68Ga-FAPI(Peking Union Medical College Hospital) Phase 1 Clinical Peking Union Medical College Hospital Neoplasm Metastasis Details
177Lu-EB-FAPI 177Lu-EB-FAPI Phase 1 Clinical Zhejiang University Pancreatic Neoplasms; Cholangiocarcinoma Details
RTX-1363-S RTX-1363S; RTX-1363-S Phase 1 Clinical Ratio Therapeutics Inc Stomach Neoplasms; Pancreatic Neoplasms; Breast Neoplasms; Lung Neoplasms Details
177Lu-DOTA-EB-FAPI Phase 1 Clinical The First Affiliated Hospital Of Xiamen University Solid tumours; Adenocarcinoma, Follicular; Thyroid Neoplasms; Thyroid Cancer, Papillary Details
68Ga/64Cu-FAPI-XT117 68Ga/64Cu-FAPI-XT117 Phase 1 Clinical Pla General Hospital Solid tumours Details
177Lu-LNC1004 177Lu-LNC1004; 177Lu-LNC-1004 Phase 1 Clinical Shanghai Lannacheng Biotechnology Co Ltd Solid tumours Details
68Ga-FAPI-RGD 68Ga-FAPI-RGD Phase 1 Clinical Peking Union Medical College Hospital Lung Neoplasms Details
SHR-7367 SHR7367; SHR-7367 Phase 1 Clinical Shanghai Hengrui Pharmaceutical Co Ltd Solid tumours; Neoplasms Details
177Lu-PNT6555(Point Biopharma) PNT-6555 Phase 1 Clinical Solid tumours; Squamous Cell Carcinoma of Head and Neck; Esophageal Neoplasms; Sarcoma; Cholangiocarcinoma; Colorectal Neoplasms; Carcinoma, Pancreatic Ductal; Melanoma Details
RO-7300490 RO-7300490; RG-6189 Phase 1 Clinical F. Hoffmann-La Roche Ltd Solid tumours; Neoplasms Details
[90Y] YFAPI-46 Clinical German Cancer Consortium (Dktk), University of Duisburg-Essen Solid tumours Details
3BP-3940 3BP-3940 Clinical Johannes Gutenberg University Of Mainz, 3B Pharmaceuticals GmbH Neoplasms Details
64Cu-LNTH-1363S 64Cu-LNTH-1363S Details
177Lu-FAP-2286 177Lu-FAP-2286 3B Pharmaceuticals GmbH Solid tumours Details

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