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FAP-2286

Cat No.:V46691 Purity: ≥98%
FAP-2286 is a potent, selective FAP-binding peptide conjugated to a radionuclide chelator, with an average FAP-binding IC50 of 2.7 nM.
FAP-2286
FAP-2286 Chemical Structure CAS No.: 2581741-18-4
Product category: New3
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
Other Sizes

Other Forms of FAP-2286:

  • FAP-2286 acetate
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
FAP-2286 is a potent, selective FAP-binding peptide conjugated to a radionuclide chelator, with an average FAP-binding IC50 of 2.7 nM. FAP-2286 is composed of a cyclic peptide that can chelate radionuclides for imaging or therapy and has strong efficacy against FAP-positive tumors. Can be used for clinical development studies in FAP-positive tumors.
Biological Activity I Assay Protocols (From Reference)
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].
ln Vivo
In the HEK-FAP tumor transplant model, FAP-2286 (30 MBq/nmol, injected intravenously) accumulates steadily [1].
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.
References

[1]. Comparative Biodistribution and Radiotherapeutic Efficacy of the Fibroblast Activation Protein (FAP)–Targeting Agents FAP-2286 and FAPI-46.

[2]. 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.

[3]. Preclinical evaluation of FAP-2286 for fibroblast activation protein targeted radionuclide imaging and therapy. Eur J Nucl Med Mol Imaging. 2022;49(11):3651-3667.

[4]. PET Imaging of Fibroblast Activation Protein in Various Types of Cancer Using 68Ga-FAP-2286: Comparison with 18F-FDG and 68Ga-FAPI-46 in a Single-Center, Prospective Study. J Nucl Med. 2023;64(3):386-394.

[5]. Preclinical evaluation of FAP-2286 for fibroblast activation protein targeted radionuclide imaging and therapy. Eur J Nucl Med Mol Imaging. 2022 Sep;49(11):3651-3667.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C67H99N13O18S3
Molecular Weight
1470.77
Exact Mass
1469.639
CAS #
2581741-18-4
Related CAS #
FAP-2286 acetate
PubChem CID
163408889
Appearance
White to off-white solid powder
LogP
-8.1
Hydrogen Bond Donor Count
12
Hydrogen Bond Acceptor Count
25
Rotatable Bond Count
25
Heavy Atom Count
101
Complexity
2760
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
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
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
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
H2O : ≥ 100 mg/mL (~67.99 mM)
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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.

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