| Identification | Back Directory | [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 | [CAS]
2581741-18-4 | [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 | [Molecular Formula]
C67H99N13O18S3 | [MOL File]
2581741-18-4.mol | [Molecular Weight]
1470.78 |
| Chemical Properties | Back Directory | [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 | [form ]
Solid | [pka]
1.83±0.10(Predicted) | [color ]
White to off-white | [Water Solubility ]
Water : ≥ 100 mg/mL (67.99 mM) |
| Hazard Information | Back Directory | [Uses]
Rofapitide 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 Activity]
FAP-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.
|
| [storage]
Store at -20°C, protect from light, stored under nitrogen | [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. |
|
| Company Name: |
Fuan Bio Gold
|
| Tel: |
15002819872 |
| Website: |
fuanbio.com / www.fuanbio.com |
|