FAP-IN-9 

FAP-IN-9 (compound P12) is a fibroblast activation protein (FAP) inhibitor with an IC₅₀ of 0.38 nM against human FAP. FAP-IN-9 functionally inhibits FAP activity, and its specific binding is verified by in vitro and in vivo blocking assays. FAP-IN-9 forms stable complexes and acts as a tumor-targeting agent. When labeled with ^99mTc, FAP-IN-9 serves as a SPECT probe and is applicable to research related to glioblastoma^[1].

FAP-IN-9 (P12) (4 pM-40 μM; 30 min (37 °C)) exhibits high binding affinity for recombinant human FAP protein, with an IC₅₀ of 0.38 nM^[1].
^99mTc-TE-FAP-IN-9 and ^99mTc-TT-FAP-IN-9 exhibit moderate hydrophilicity, with LogP values of -2.78 and -3.27, respectively^[1].
^99mTc-TE-FAP-IN-9 and ^99mTc-TT-FAP-IN-9 (37 MBq; 6 h (PBS, room temp); 6 h (human blood serum, 37 °C)) demonstrate excellent in vitro stability, with radiochemical purity remaining above 95% after 6 h of incubation in PBS at room temperature or human blood serum at 37 °C^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

^99mTc-TE-P12 and ^99mTc-TT-P12, derivatives of FAP-IN-9 (P12) (3.7 MBq; i.v.; single dose), exhibit high, FAP-specific tumor uptake in U87MG glioblastoma-bearing mice, with ^99mTc-TT-P12 showing the highest tumor uptake (44.86 %ID/g at 60 minutes p.i.) and sustained retention over 4 hours, while both agents achieve high tumor-to-nontarget tissue ratios suitable for SPECT imaging^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1284.31

C₅₇H₇₆F₂N₉NaO₁₉S

O=C(NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCC(NC1=CC=CC2=C1N=CC=C2C(NCC(N3CC(C[C@@H]3C#N)(F)F)=O)=O)=O)C4=CC=C(N/N=C/C5=C(S(=O)(O[Na])=O)C=CC=C5)N=C4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Sufan Tang, et al. Synthesis
  and In Vivo and In Vitro Properties
  of ^99mTc-Labeled Fibroblast
  Activation Protein Inhibitors. Mol. Pharmaceutics 2026, 23, 2752−2765.