| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
FAP-2286 targets Fibroblast Activation Protein (FAP), a cell surface serine protease highly expressed on cancer-associated fibroblasts (CAFs) in many epithelial tumors. The mean IC50 for FAP binding is 1.3-2.7 nM.
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|---|---|
| ln Vitro |
The human WI-38 fibroblast-like fetal lung line is less susceptible to the binding of fluorophore-labeled competing peptides when FAP-2286 (0.1-30 nM, 1 hour) is applied [1]. In HEK-FAP cells, FAP-2286 (5 nM, 1, 3, 8, 24, and 72 hours) allows for extended tumor retention and inhibition [1].
FAP-2286 demonstrates high binding affinity and selectivity for FAP. It can be radiolabeled with diagnostic isotopes (e.g., ⁶⁸Ga) for PET imaging to visualize FAP-expressing tumors. It can also be labeled with therapeutic isotopes (e.g., ¹⁷⁷Lu) for targeted radionuclide therapy. |
| ln Vivo |
In the HEK-FAP tumor transplant model, FAP-2286 (30 MBq/nmol, injected intravenously) accumulates steadily [1].
⁶⁸Ga-FAP-2286 PET imaging demonstrates high tumor uptake and excellent contrast for detecting primary and metastatic lesions in patients with various cancers, including pancreatic, colorectal, and lung cancer. ¹⁷⁷Lu-FAP-2286 shows antitumor activity in preclinical models and early clinical studies. |
| Enzyme Assay |
Surface Plasmon Resonance (SPR) or radio-ligand binding assays using recombinant FAP protein are used to measure binding affinity (Kd, IC50). The labeled compound's binding to FAP-expressing cells is confirmed via autoradiography or gamma counting.
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| Cell Assay |
FAP-expressing cancer-associated fibroblast cell lines are incubated with radiolabeled FAP-2286. Specific binding is determined by competition with excess unlabeled compound. Internalization assays are performed by incubating cells at 37degC, then stripping surface-bound activity and measuring internalized radioactivity.
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| Animal Protocol |
Animal/Disease Models: HEK-FAP tumor-bearing mice[1]
Doses: 30 MBq/nmol Route of Administration: intravenous (iv) (iv)injection Experimental Results: Tumor to kidney (T/K) ratio increased, with the highest differential uptake obtained 48 hrs (hrs (hours)) after injection 7.5 T/K. The cumulative dose was maintained at 10.8 ID/g 3 hrs (hrs (hours)) after injection. In PET imaging studies, patients or animals are injected with ⁶⁸Ga-FAP-2286 intravenously. PET/CT scans are performed at specific time points post-injection. For therapy, animals with xenograft tumors receive ¹⁷⁷Lu-FAP-2286 intravenously, and tumor growth is monitored. |
| ADME/Pharmacokinetics |
As a radiolabeled peptide, the PK of FAP-2286 is characterized by rapid blood clearance and high tumor accumulation. The DOTA chelator ensures stable complexation of radiometals. Biodistribution studies show predominant renal excretion.
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| Toxicity/Toxicokinetics |
For therapeutic applications (¹⁷⁷Lu-FAP-2286), the primary toxicity concern is off-target radiation exposure to normal tissues, particularly the kidneys, bone marrow, and salivary glands. Hematological parameters are monitored for bone marrow toxicity.
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| References |
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| Additional Infomation |
FAP-2286 is a clinical-stage theranostic agent (diagnosis and therapy). It is being evaluated in clinical trials for various cancers. Theranostic agents allow precise patient selection by confirming target expression with PET imaging before administering radionuclide therapy.
|
| Molecular Formula |
C67H99N13O18S3
|
|---|---|
| Molecular Weight |
1470.77
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| Exact Mass |
1469.639
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| CAS # |
2581741-18-4
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| Related CAS # |
FAP-2286 acetate
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| PubChem CID |
163408889
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| Appearance |
White to off-white solid powder
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| LogP |
-8.1
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
25
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| Rotatable Bond Count |
25
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| Heavy Atom Count |
101
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| Complexity |
2760
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| Defined Atom Stereocenter Count |
8
|
| SMILES |
CCCCCC(=O)N[C@H]1CSCC2=CC(=CC(=C2)CSCCNC(=O)CN3CCN(CCN(CCN(CC3)CC(=O)O)CC(=O)O)CC(=O)O)CSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]4CCCN4C(=O)[C@@H]5CCCN5C1=O)[C@@H](C)O)CCC(=O)N)CC6=CC=CC=C6)C(=O)O
|
| InChi Key |
UHKLVUPDBJFFBB-ZCDGVBLYSA-N
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| InChi Code |
InChI=1S/C67H99N13O18S3/c1-3-4-6-15-55(83)70-50-41-100-39-46-30-45(38-99-29-18-69-56(84)34-75-21-23-76(35-57(85)86)25-27-78(37-59(89)90)28-26-77(24-22-75)36-58(87)88)31-47(32-46)40-101-42-51(67(97)98)73-62(92)49(33-44-11-7-5-8-12-44)72-61(91)48(16-17-54(68)82)71-64(94)60(43(2)81)74-63(93)52-13-9-19-79(52)66(96)53-14-10-20-80(53)65(50)95/h5,7-8,11-12,30-32,43,48-53,60,81H,3-4,6,9-10,13-29,33-42H2,1-2H3,(H2,68,82)(H,69,84)(H,70,83)(H,71,94)(H,72,91)(H,73,92)(H,74,93)(H,85,86)(H,87,88)(H,89,90)(H,97,98)/t43-,48+,49+,50+,51+,52+,53+,60+/m1/s1
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| Chemical Name |
(5R,11S,17S,20S,23S,26S,29R)-23-(3-amino-3-oxopropyl)-26-benzyl-5-(hexanoylamino)-20-[(1R)-1-hydroxyethyl]-6,12,18,21,24,27-hexaoxo-35-[2-[[2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetyl]amino]ethylsulfanylmethyl]-3,31-dithia-7,13,19,22,25,28-hexazatetracyclo[31.3.1.07,11.013,17]heptatriaconta-1(37),33,35-triene-29-carboxylic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ≥ 100 mg/mL (~67.99 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (34.00 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT04939610
Conditions:Solid TumorLink: https://clinicaltrials.gov/ct2/show/NCT07434180
Conditions:Cancer of Unknown PrimaryProducts are for research use only; We do not sell to patients
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