[CAS NO. 2581741-18-4] FAP-2286
PRODUCTS SPECIFICATIONS [2581741-18-4]
DESCRIPTION [2581741-18-4]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 1470.77 |
| Molecular Formula | C67H99N13O18S3 |
| SMILES | O=C(N1[C@@](C(N[C@@](C(N[C@H](C(N[C@H](C2=O)CC3=CC=CC=C3)=O)CCC(N)=O)=O)([H])[C@H](O)C)=O)([H])CCC1)[C@@](CCC4)([H])N4C([C@H](CSCC5=CC(CSCCNC(CN(CCN(CC6)CC(O)=O)CCN(CCN6CC(O)=O)CC(O)=O)=O)=CC(CSC[C@H](N2)C(O)=O)=C5)NC(CCCCC)=O)=O |
Summary
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 K d 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] .
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04621435 | Thomas Hope|Clovis Oncology, Inc.|University of California, San Francisco |
Solid Tumors, Adult|Metastatic Cancer
|
December 14, 2020 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
H 2 O : ≥ 100 mg/mL ( 67.99 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.6799 mL | 3.3996 mL | 6.7992 mL |
| 5 mM | 0.1360 mL | 0.6799 mL | 1.3598 mL |
| 10 mM | 0.0680 mL | 0.3400 mL | 0.6799 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (34.00 mM); Clear solution; Need ultrasonic
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.
