| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
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| 50mg | |||
| 100mg |
| Targets |
FAP (fibroblast activation protein)
NOTA-FAPI-46 targets fibroblast activation protein (FAP). FAP is a serine protease that is highly expressed in cancer-associated fibroblasts (CAFs) within the tumor microenvironment. The mechanism of action for NOTA-FAPI-46 involves selective binding to FAP on the surface of activated fibroblasts within tumors. The NOTA chelator allows for radiolabeling with PET isotopes. |
|---|---|
| ln Vitro |
In vitro, NOTA-FAPI-46 is expected to show high affinity and specificity for FAP, similar to FAPI-46. The compound's affinity for FAP is typically measured using surface plasmon resonance or binding assays on FAP-expressing cells. These in vitro activities support its use as a PET tracer for imaging FAP expression.
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| ln Vivo |
In vivo, NOTA-FAPI-46 can be used as a PET tracer to identify conditions where FAP overexpression is present. When labeled with a suitable radioisotope, such as ⁶⁸Ga or ¹⁸F, it can be used for PET imaging of FAP-positive tumors. [¹⁸F]AlF-NOTA-GL01, an improved FAPI-46 derivative, has been studied from preclinical to first-in-human.
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| Enzyme Assay |
The in vitro FAP binding assay for NOTA-FAPI-46 is conducted using FAP-expressing cell lines. Cells are incubated with radiolabeled NOTA-FAPI-46 (e.g., ⁶⁸Ga-NOTA-FAPI-46). The bound radioactivity is measured, and the binding affinity (Kd) is calculated. Competitive binding assays are performed using unlabeled FAPI ligands to confirm specificity. Cellular uptake and internalization studies are also performed.
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| Cell Assay |
Cellular uptake assays for NOTA-FAPI-46 are performed using FAP-positive cells. Cells are incubated with radiolabeled NOTA-FAPI-46 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. The uptake is expressed as a percentage of the added dose per milligram of protein.
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| Animal Protocol |
In vivo imaging studies for NOTA-FAPI-46 are conducted in mouse models bearing FAP-positive tumor xenografts. The radiolabeled compound (e.g., ⁶⁸Ga-NOTA-FAPI-46 or [¹⁸F]AlF-NOTA-GL01) is administered via intravenous injection. PET/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 NOTA-FAPI-46 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 NOTA-FAPI-46 is not extensively reported. As a research compound, NOTA-FAPI-46 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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| Additional Infomation |
NOTA-FAPI-46 is an analog of FAPI-46 that incorporates a NOTA chelator for radiolabeling with PET isotopes. It targets fibroblast activation protein (FAP) and is used in medical imaging and cancer diagnostics. When labeled with ⁶⁸Ga or ¹⁸F, it can be used for PET imaging of FAP-positive tumors. It is for research use only.
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| Molecular Formula |
C37H50F2N10O7
|
|---|---|
| Molecular Weight |
566.612
|
| Exact Mass |
784.3832
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| Elemental Analysis |
C, 56.62; H, 6.42; F, 4.84; N, 17.85; O, 14.27
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| Appearance |
Typically exists as solid at room temperature
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| InChi Key |
APILFOLSMKOIDY-NDEPHWFRSA-N
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| InChi Code |
InChI=1S/C37H50F2N10O7/c1-43(27-3-4-31-30(19-27)29(5-6-41-31)36(56)42-22-32(50)49-26-37(38,39)20-28(49)21-40)7-2-8-44-15-17-48(18-16-44)33(51)23-45-9-11-46(24-34(52)53)13-14-47(12-10-45)25-35(54)55/h3-6,19,28H,2,7-18,20,22-26H2,1H3,(H,42,56)(H,52,53)(H,54,55)/t28-/m0/s1
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| Chemical Name |
(S)-2,2'-(7-(2-(4-(3-((4-((2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl)carbamoyl)quinolin-6-yl)(methyl)amino)propyl)piperazin-1-yl)-2-oxoethyl)-1,4,7-triazonane-1,4-diyl)diacetic acid
|
| Synonyms |
NOTA-FAPI-46; NOTA-FAPI 46; NOTA-FAPI46;
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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 | 1.7649 mL | 8.8244 mL | 17.6488 mL | |
| 5 mM | 0.3530 mL | 1.7649 mL | 3.5298 mL | |
| 10 mM | 0.1765 mL | 0.8824 mL | 1.7649 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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