| Identification | Back Directory | [Name]
(S)-4-((4-((2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl)carbamoyl)quinolin-8-yl)amino)-4-oxobutanoic acid | [CAS]
2639365-69-6 | [Synonyms]
(S)-4-((4-((2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl)carbamoyl)quinolin-8-yl)amino)-4-oxobutanoic acid | [Molecular Formula]
C21H19F2N5O5 | [MOL File]
2639365-69-6.mol | [Molecular Weight]
459.4 |
| Chemical Properties | Back Directory | [Boiling point ]
913.5±65.0 °C(Predicted) | [density ]
1.50±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
4.52±0.10(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential. | [Biological Activity]
OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential. | [in vivo]
177Lu-OncoFAP-DOTAGA (50 nmol/kg - 1 μmol/kg, i.v., single dose) efficiently targets FAP-positive tumors in the SK-RC-52.hFAP xenograft model, with dose-dependent accumulation[1]. | Animal Model: | Xenograft model of humanized FAP renal cancer (SK-RC-52.hFAP) in nude mice[1] | | Dosage: |
50, 125, 250, 500 nmol/kg, and 1 μmol/kg (in the form of 177Lu-OncoFAP-DOTAGA) | | Administration: | Intravenous injection (i.v.), single dose | | Result: | Reached 32% of the injected dose per gram of tumor tissue (ID/g) within 10 minutes and maintained above 20% ID/g for 6 hours. |
| [References]
[1]. Millul J, et al. An ultra-high-affinity small organic ligand of fibroblast activation protein for tumor-targeting applications. Proc Natl Acad Sci U S A. 2021 Apr 20;118(16):e2101852118. |
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