FAP-2286 is a potent and selective FAP-binding peptide coupled to a radionuclide chelator with a mean IC50 value of 2.7 nM for binding to FAP. FAP-2286 consists of two functional elements: a FAP-targeting peptide and a chelator used to attach radioisotopes. FAP-2286 and its metal complexes demonstrated high affinity to FAP recombinant protein and cell surface FAP expressed on fibroblasts. Biodistribution studies in mice showed rapid and persistent uptake of 68Ga-FAP-2286, 111In-FAP-2286, and 177Lu-FAP-2286 in FAP-positive tumors, with renal clearance and minimal uptake in normal tissues. 177Lu-FAP-2286 exhibited antitumor activity in FAP-expressing HEK293 tumors and sarcoma patient-derived xenografts, with no significant weight loss. In addition, FAP-2286 maintained longer tumor retention and suppression in comparison to FAPI-46.
MedKoo Cat#: 207200
Name: FAP-2286
CAS#: 2581741-18-4
Chemical Formula: C67H99N13O18S3
Exact Mass: 1469.6393
Molecular Weight: 1470.78
Elemental Analysis: C, 54.71; H, 6.78; N, 12.38; O, 19.58; S, 6.54
The following data is based on the product molecular weight 1,470.78 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
