L-Cysteine, S-[[3-(mercaptomethyl)-5-[[[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]ethyl]thio]methyl]phenyl]methyl]-N-(1-oxohexyl)-L-cysteinyl-L-prolyl-L-prolyl-L-threonyl-L-glutaminyl-L-phenylalanyl-, cyclic (1→7)-thioethe

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L-Cysteine, S-[[3-(mercaptomethyl)-5-[[[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]ethyl]thio]methyl]phenyl]methyl]-N-(1-oxohexyl)-L-cysteinyl-L-prolyl-L-prolyl-L-threonyl-L-glutaminyl-L-phenylalanyl-, cyclic (1→7)-thioether Suppliers list
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L-Cysteine, S-[[3-(mercaptomethyl)-5-[[[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]ethyl]thio]methyl]phenyl]methyl]-N-(1-oxohexyl)-L-cysteinyl-L-prolyl-L-prolyl-L-threonyl-L-glutaminyl-L-phenylalanyl-, cyclic (1→7)-thioether manufacturers
L-Cysteine, S-[[3-(mercaptomethyl)-5-[[[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]ethyl]thio]methyl]phenyl]methyl]-N-(1-oxohexyl)-L-cysteinyl-L-prolyl-L-prolyl-L-threonyl-L-glutaminyl-L-phenylalanyl-, cyclic (1→7)-thioether Basic information
Product Name:L-Cysteine, S-[[3-(mercaptomethyl)-5-[[[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]ethyl]thio]methyl]phenyl]methyl]-N-(1-oxohexyl)-L-cysteinyl-L-prolyl-L-prolyl-L-threonyl-L-glutaminyl-L-phenylalanyl-, cyclic (1→7)-thioether
Synonyms:L-Cysteine, S-[[3-(mercaptomethyl)-5-[[[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]ethyl]thio]methyl]phenyl]methyl]-N-(1-oxohexyl)-L-cysteinyl-L-prolyl-L-prolyl-L-threonyl-L-glutaminyl-L-phenylalanyl-, cyclic (1→7)-thioether;FAP-2286，FAP2286;2,2',2''-(10-(2-((2-((((12S,32S,5R,13R,16S,19S,22S)-19-(3-Amino-3-oxopropyl)-16-benzyl-13-carboxy-5-hexanamido-22-((R)-1-hydroxyethyl)-2,4,15,18,21,24-hexaoxo-7,11-dithia-14,17,20,23-tetraaza-1(1,2),3(2,1)-dipyrrolidina-9(1,3)-benzenacyclotetracosaphane-95-yl)methyl)thio)ethyl)amino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid;Rofapitide tetraxetan;FAPI-2286
CAS:2581741-18-4
MF:C67H99N13O18S3
MW:1470.78
EINECS:
Product Categories:
Mol File:2581741-18-4.mol
L-Cysteine, S-[[3-(mercaptomethyl)-5-[[[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]ethyl]thio]methyl]phenyl]methyl]-N-(1-oxohexyl)-L-cysteinyl-L-prolyl-L-prolyl-L-threonyl-L-glutaminyl-L-phenylalanyl-, cyclic (1→7)-thioether Structure
L-Cysteine, S-[[3-(mercaptomethyl)-5-[[[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]ethyl]thio]methyl]phenyl]methyl]-N-(1-oxohexyl)-L-cysteinyl-L-prolyl-L-prolyl-L-threonyl-L-glutaminyl-L-phenylalanyl-, cyclic (1→7)-thioether Chemical Properties
Boiling point 1678.6±65.0 °C(Predicted)
density 1.42±0.1 g/cm3(Predicted)
storage temp. Store at -20°C, protect from light, stored under nitrogen
pka1.83±0.10(Predicted)
form Solid
color White to off-white
Water Solubility Water : ≥ 100 mg/mL (67.99 mM)
Safety Information
MSDS Information
L-Cysteine, S-[[3-(mercaptomethyl)-5-[[[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]ethyl]thio]methyl]phenyl]methyl]-N-(1-oxohexyl)-L-cysteinyl-L-prolyl-L-prolyl-L-threonyl-L-glutaminyl-L-phenylalanyl-, cyclic (1→7)-thioether Usage And Synthesis
UsesRofapitide tetraxetan (FAP-2286) is a potent and selective FAP-binding peptide with a mean IC50 value of 2.7 nM for binding to FAP. Rofapitide tetraxetan can be labeled with radionuclides for diagnostic applications. Rofapitide tetraxetan has antitumor activity[1].
Biological ActivityFAP-2286, a fibroblast activation protein (FAP)-binding peptidic macrocycle coupled to the radionuclide chelator DOTA. FAP-2286 has potent affinity to human FAP protein with a Kd of 1.1 nM. FAP-2286, a tumor imaging agent, is a useful tool for the research of positron emission tomography (PET). FAP-2286 has antitumor activity[1][2].
in vivo

Rofapitide tetraxetan (30 MBq/nmol for intravenous injection) accumulated atably maintained in the tumors of HEK-FAP tumor-bearing mice[1].

Animal Model:HEK-FAP tumor-bearing mice[1]
Dosage:30 MBq/nmol
Administration:Intravenous injection (i.v.)
Result:Increased tumor-to-kidney (T/K) ratio with the highest differential uptake of 7.5 T/K obtained at 48 h post injection.
Maintained accumulation at 3 h after injection with 10.8 ID/g.
References[1]. Dirk Zboralski, et al. Comparative Biodistribution and Radiotherapeutic Efficacy of the Fibroblast Activation Protein (FAP)-Targeting Agents FAP-2286 and FAPI-46.[2]. Richard P Baum, et al. Feasibility, Biodistribution, and Preliminary Dosimetry in Peptide-Targeted Radionuclide Therapy of Diverse Adenocarcinomas Using 177 Lu-FAP-2286: First-in-Humans Results. J Nucl Med. 2022 Mar;63(3):415-423.
L-Cysteine, S-[[3-(mercaptomethyl)-5-[[[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]ethyl]thio]methyl]phenyl]methyl]-N-(1-oxohexyl)-L-cysteinyl-L-prolyl-L-prolyl-L-threonyl-L-glutaminyl-L-phenylalanyl-, cyclic (1→7)-thioether Preparation Products And Raw materials
Tag:L-Cysteine, S-[[3-(mercaptomethyl)-5-[[[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]ethyl]thio]methyl]phenyl]methyl]-N-(1-oxohexyl)-L-cysteinyl-L-prolyl-L-prolyl-L-threonyl-L-glutaminyl-L-phenylalanyl-, cyclic (1→7)-thioether(2581741-18-4) Related Product Information
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