| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
Purity: =99.84%
| Targets |
FAP (fibroblast activation protein)
HYNIC-FAPI-04 targets fibroblast activation protein (FAP). FAP is a serine protease that is overexpressed on cancer-associated fibroblasts (CAFs) within the tumor microenvironment. The HYNIC chelator allows for the attachment of ⁹⁹ᵐTc, a widely used radioisotope for SPECT imaging. By binding to FAP, HYNIC-FAPI-04 enables the visualization of FAP-positive tumors. |
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| ln Vitro |
In vitro cell uptake experiments of 99mTc-HYNIC-FAPI-04 showed good FAP binding specificity, and the cellular uptake significantly decreased when blocked by DOTA-FAPI-04, reflecting the similar targeting mechanism of HYNIC-FAPI-04 and DOTA-FAPI-04.[1]
In vitro, HYNIC-FAPI-04 shows good FAP binding specificity. Cellular uptake experiments demonstrate that the compound specifically binds to FAP-expressing cells, and the cellular uptake significantly decreases when blocked by DOTA-FAPI-04. This reflects the similar targeting mechanism of HYNIC-FAPI-04 and DOTA-FAPI-04. The compound shows excellent affinity and specificity for FAP. |
| ln Vivo |
SPECT/CT imaging showed that U87MG tumor was distinguishable and of a high uptake of 99mTc-HYNIC-FAPI-04 (2.67 ± 0.35 %ID/mL at 1.5 h post injection (h P.I.), while tumor signal of FAP-negative HUH-7 was as low as 0.34 ± 0.06 %ID/mL. At 5 h P.I., U87MG tumor was still distinguishable (1.81 ± 0.20 %ID/mL). In comparison, although U87MG tumor was of obvious 68Ga-FAPI-04 uptake and clearly visible at 1 h P.I., the tumorous radioactive signals were fuzzy at 1.5 h P.I. 99mTc-HYNIC-FAPI-04 specifically bound to FAP-positive tumors and qualified with the ability of evaluating tumor fibrosis over longer time windows.[1]
In vivo, ⁹⁹ᵐTc-HYNIC-FAPI-04 is a promising SPECT radiotracer for (re)staging and treatment planning of breast cancers. It has been developed as a FAPI-based radiotracer for tumor imaging. The radiotracer shows excellent affinity and specificity for FAP in preclinical studies. However, specific published in vivo efficacy studies are not detailed in the current literature. |
| Enzyme Assay |
The in vitro FAP binding assay for HYNIC-FAPI-04 is conducted using FAP-expressing cell lines. Cells are incubated with radiolabeled HYNIC-FAPI-04 (⁹⁹ᵐTc-HYNIC-FAPI-04). The bound radioactivity is measured, and the binding affinity is calculated. Competitive binding assays are performed using unlabeled FAPI ligands (e.g., DOTA-FAPI-04) to confirm specificity. Cellular uptake and internalization studies are also performed.
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| Cell Assay |
Cellular uptake assays for HYNIC-FAPI-04 are performed using FAP-positive cells. Cells are incubated with ⁹⁹ᵐTc-HYNIC-FAPI-04 at 37°C. The cells are washed, and the internalized radioactivity is measured. The specificity of uptake is confirmed by blocking with an excess of unlabeled ligand (e.g., DOTA-FAPI-04). The uptake is expressed as a percentage of the added dose.
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| Animal Protocol |
In vivo imaging studies for HYNIC-FAPI-04 are conducted in mouse models bearing FAP-positive tumor xenografts. The radiolabeled compound (⁹⁹ᵐTc-HYNIC-FAPI-04) is administered via intravenous injection. SPECT/CT imaging is performed at various time points post-injection to visualize the biodistribution and tumor uptake of the tracer. The tumor-to-background ratio is calculated to assess the imaging contrast.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for HYNIC-FAPI-04 is not extensively reported in publicly available sources. The pharmacokinetic properties depend on the specific radioisotope and the formulation used. For radiolabeled compounds, the biodistribution and clearance are typically evaluated in animal models. Detailed PK parameters such as half-life and bioavailability are not available in the current literature.
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| Toxicity/Toxicokinetics |
Toxicity data for HYNIC-FAPI-04 is not extensively reported. As a research compound, HYNIC-FAPI-04 is intended for research use only and not for human therapeutic applications. The toxicity would depend on the specific radioisotope used for labeling. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References |
[1]. SPECT Imaging with Tc-99m-Labeled HYNIC-FAPI-04 to Extend the Differential Time Window in Evaluating Tumor Fibrosis. Pharmaceuticals (Basel). 2023 Mar 10;16(3):423.
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| Additional Infomation |
HYNIC-FAPI-04 is a FAPI-04-derived radiotracer that targets fibroblast activation protein (FAP). It is designed for radiolabeling with ⁹⁹ᵐTc for SPECT imaging of tumors. It shows excellent affinity and specificity for FAP and is a promising SPECT radiotracer for breast cancer imaging. It is for research use only.
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| Molecular Formula |
C31H34F2N8O4
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|---|---|
| Molecular Weight |
620.66
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| Exact Mass |
620.27
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| Elemental Analysis |
C, 59.99; H, 5.52; F, 6.12; N, 18.05; O, 10.31
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| Appearance |
Typically exists as solid at room temperature
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| SMILES |
O=C(C1=CC=NC2=CC=C(OCCCN3CCN(C(C4=CC=C(NN)C=C4)=O)CC3)C=C12)NCC(N5[C@H](C#N)CC(F)(F)C5)=O
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| InChi Key |
COFGLVCKAJLHSU-QHCPKHFHSA-N
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| InChi Code |
InChI=1S/C31H34F2N8O4/c32-31(33)17-23(18-34)41(20-31)28(42)19-37-29(43)25-8-9-36-27-7-6-24(16-26(25)27)45-15-1-10-39-11-13-40(14-12-39)30(44)21-2-4-22(38-35)5-3-21/h2-9,16,23,38H,1,10-15,17,19-20,35H2,(H,37,43)/t23-/m0/s1
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| Chemical Name |
N-[2-[(2S)-2-cyano-4,4-difluoropyrrolidin-1-yl]-2-oxoethyl]-6-[3-[4-(4-hydrazinylbenzoyl)piperazin-1-yl]propoxy]quinoline-4-carboxamide
InChi Key: COFGLVCKAJLHSU-QHCPKHFHSA-N
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| Synonyms |
HYNIC-FAPI-04; HYNIC FAPI-04; HYNIC-FAPI 04; HYNIC FAPI 04; HYNIC-FAPI-4
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6112 mL | 8.0559 mL | 16.1119 mL | |
| 5 mM | 0.3222 mL | 1.6112 mL | 3.2224 mL | |
| 10 mM | 0.1611 mL | 0.8056 mL | 1.6112 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.
Products are for research use only; We do not sell to patients
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