| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
| Targets |
Melanin probe-2 is a precursor that is itself not directly active as a PET probe. Its target is the enzyme or chemical labeling system required to incorporate the radionuclide Fluorine-18 (¹⁸F). The final ¹⁸F-labeled product targets melanin, a pigment found in high concentrations in melanomas. The probe binds specifically to melanin with high affinity, allowing PET visualization of tumor tissue.
|
|---|---|
| ln Vitro |
The in vitro activity of Melanin probe-2 is its ability to serve as a substrate for the nucleophilic radiofluorination reaction. It contains a bromine leaving group that can be efficiently replaced by the [¹⁸F]fluoride ion. The reaction yield and radiochemical purity of the final PET probe are the key metrics of its in vitro performance.
|
| ln Vivo |
Melanin probe-2 itself has no direct in vivo activity. The in vivo activity resides in the ¹⁸F-labeled picolinamide probe synthesized from it. This radiolabeled probe accumulates in melanin-rich tissues. In a mouse model of malignant melanoma, the ¹⁸F-labeled probe shows high tumor uptake and slow clearance, providing high-contrast PET images of the melanoma.
|
| Enzyme Assay |
A non-cellular radiolabeling reaction is the primary experimental workflow. A solution of Melanin probe-2 (precursor) in a polar aprotic solvent (e.g., DMF or DMSO) is added to a dried [¹⁸F]fluoride/K2CO3/Kryptofix 222 mixture. The reaction is heated to 100-130degC for 10-20 minutes. The crude reaction mixture is then analyzed by radio-TLC and radio-HPLC to determine the radiochemical yield (RCY) and purity, which is the main readout of the experiment.
|
| Cell Assay |
Melanin probe-2 is a reagent used in a chemistry lab, not a drug tested on cells. The final ¹⁸F-labeled picolinamide probe is tested in cellular uptake assays. Melanoma cells (e.g., B16F10 mouse melanoma cells) are incubated with the radiolabeled probe in culture medium. After 30-60 minutes, cells are washed, lysed, and the accumulated radioactivity is measured using a gamma counter to determine the probe‘s binding specificity and affinity for melanin.
|
| Animal Protocol |
For in vivo evaluation, the ¹⁸F-labeled picolinamide probe synthesized from the precursor is injected intravenously (tail vein) into a mouse model of subcutaneous B16F10 melanoma (tumor-bearing nude mice). At various time points (e.g., 15 min, 30 min, 1 h, 2 h), the mice undergo a PET/CT scan. After the final scan, the mice are euthanized, and major organs (tumor, muscle, blood, liver) are harvested to measure radioactivity biodistribution in a gamma counter. Tumor-to-background ratios are calculated to assess the probe‘s efficacy for imaging.
|
| ADME/Pharmacokinetics |
Melanin probe-2 is a small organic molecule. As a synthetic precursor, its absorption and metabolism are not studied. For the final radiolabeled PET probe, PK is characterized by analyzing blood samples collected from mice at various time points after injection. The probe is typically cleared rapidly from the blood (t1/2 = minutes) through renal and hepatobiliary excretion. The ¹⁸F isotope has a physical half-life of 109.8 minutes.
|
| Toxicity/Toxicokinetics |
Specific toxicity studies are not applicable to the non-radioactive precursor. For the final ¹⁸F-labeled PET probe, the compound is administered as a single microdose (< 10-⁹ g/kg for the mass of the drug, though with high radioactive dose). At these ultra-low mass doses, there is no pharmacologically-induced toxicity. The primary risk is from the ionizing radiation, which is minimized for research by using the lowest feasible dose.
|
| References |
[1]. Liu H, et al. Development of 18F-labeled picolinamide probes for PET imaging of malignant melanoma. J Med Chem. 2013;56(3):895‐901.
|
| Additional Infomation |
Melanin probe-2 (compound 5) was developed by researchers to create a better PET tracer for melanoma. The final ¹⁸F-labeled picolinamide probe has advantages over older tracers (like ¹⁸F-FDG) due to its high specificity for melanin, reducing false positives from inflammation. As a precursor, it is not an approved drug. It is a chemical intermediate for research use only.
|
| Molecular Formula |
C12H18BRN3O
|
|---|---|
| Molecular Weight |
300.1948
|
| Exact Mass |
299.063
|
| CAS # |
1285446-04-9
|
| PubChem CID |
62952677
|
| Appearance |
Light yellow to yellow oil
|
| LogP |
1.9
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
17
|
| Complexity |
234
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCN(CC)CCNC(=O)C1=NC=C(C=C1)Br
|
| InChi Key |
BSMXWXBEJYOUAH-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H18BrN3O/c1-3-16(4-2)8-7-14-12(17)11-6-5-10(13)9-15-11/h5-6,9H,3-4,7-8H2,1-2H3,(H,14,17)
|
| Chemical Name |
5-bromo-N-[2-(diethylamino)ethyl]pyridine-2-carboxamide
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 125 mg/mL (416.40 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (20.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 6.25 mg/mL (20.82 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3312 mL | 16.6561 mL | 33.3122 mL | |
| 5 mM | 0.6662 mL | 3.3312 mL | 6.6624 mL | |
| 10 mM | 0.3331 mL | 1.6656 mL | 3.3312 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
