| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
The primary target of EC-17 sodium is the folate receptor alpha (FRα), a glycosylphosphatidylinositol (GPI)-anchored cell surface protein that binds folate with high affinity. FRα is a well-established tumor-associated antigen, as it is overexpressed on the surfaces of many cancer cells, including those of ovarian, lung, breast, and kidney cancers, while its expression in normal tissues is highly restricted. This differential expression pattern makes FRα an attractive target for tumor-specific imaging and therapy. Upon administration, the folate moiety of EC-17 sodium binds to FRα on the cancer cell surface. This binding allows for the selective accumulation of the fluorescent conjugate in tumor tissues. The compound's fluorescent properties, with peak excitation and emission at 470/520 nm, enable the visualization of FRα-expressing cells. In addition to its role as an imaging agent, EC-17 sodium can also facilitate therapeutic effects. Once bound to the cancer cell via the folate moiety, circulating anti-fluorescein antibodies can recognize and bind to the FITC moiety of the conjugate, resulting in antibody-dependent cellular cytotoxicity (ADCC). This mechanism leverages the patient's immune system to eliminate FRα-positive tumor cells. The specific targeting of FRα by EC-17 sodium thus provides a dual mechanism for both cancer diagnosis and treatment.
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| ln Vitro |
The spectral binding wavelength of fluorescein, which is present in EC-17 disodium salt, is 490-530 nm. By using an ethylenediamine spacer to combine folic acid (vitamin B9) with fluorescein isothiocyanate (FITC), EC-17 disodium salt is created. Folic acid-FITC has a molecular weight of 917 kDa. FITC is a fluorescein gel that has reactive isothiocyanate groups functionalized in it. The chemical known as folic acid-FITC conjugate is fluorescent and negatively charged, and it is used to electrophorese the cell surface of FRα EC-17 disodium salt on HeLa cells. Depending on the molar concentration of Mal and concentration, the signal-to-background ratio (SBR) on HeLa cells varies from 0.97 to 7.32[1].
EC-17 sodium exhibits specific in vitro activity by binding to folate receptors on cancer cells. The compound is a conjugate of fluorescein isothiocyanate (FITC) and folic acid, which allows it to bind to folate receptor alpha (FRα) that is overexpressed on the surface of many cancer cell lines, including HeLa, KB, and various ovarian and breast cancer cells. The binding affinity is mediated by the folate moiety, which has a high affinity for FRα. Upon binding, the FITC moiety provides a fluorescent signal that can be detected and quantified. The spectral binding wavelength of fluorescein in EC-17 is in the range of 490-530 nm, and the signal-to-background ratio (SBR) on HeLa cells varies from 0.97 to 7.32 depending on the concentration of the compound. This concentration-dependent fluorescence allows for the sensitive detection of FRα-positive cells. In vitro studies also demonstrate that EC-17 sodium can facilitate antibody-dependent cellular cytotoxicity (ADCC). When FRα-positive cells are incubated with EC-17 sodium in the presence of anti-fluorescein antibodies, the antibodies bind to the FITC moiety of the cell-bound conjugate, leading to the recruitment of immune effector cells and subsequent target cell lysis. This dual functionality makes EC-17 sodium a valuable tool for both imaging and therapeutic applications in vitro. |
| ln Vivo |
Animals injected with EC-17 disodium salt had an average fluorescence signal of 42,234 ± 12,234 au [1]. Folate-FITC fluorescence microscopy reveals no signal in FR-α-negative or benign lesions and a high signal in all cancers expressing FR-α [2].
In vivo, EC-17 sodium functions as a fluorescent contrast agent for the detection and imaging of tumors that overexpress folate receptor alpha (FRα). Animals injected with EC-17 disodium salt exhibit an average fluorescence signal of 42,234 ± 12,234 au, indicating a strong and specific accumulation of the compound in tumor tissues. Folate-FITC fluorescence microscopy reveals no signal in FR-α-negative or benign lesions, while a high signal is observed in all cancers expressing FR-α. This high specificity allows for the clear delineation of tumor margins and the identification of metastatic lesions during surgical procedures. The compound's fluorescent properties in the visible light spectrum enable real-time imaging and tumor localization. By selectively binding to FRα, EC-17 enhances the visualization of cancerous tissues while sparing normal cells, which typically have low or no FRα expression. This property is particularly valuable for intraoperative guidance, helping surgeons to achieve complete tumor resection. In addition to imaging, EC-17 sodium has potential therapeutic applications in vivo. Once bound to the cancer cell through the folate moiety, circulating anti-fluorescein antibodies can recognize and bind to the FITC moiety, resulting in antibody-dependent cellular cytotoxicity (ADCC). This immune-mediated mechanism can contribute to the elimination of tumor cells, providing a combined diagnostic and therapeutic approach. |
| Enzyme Assay |
The in vitro assay for EC-17 sodium typically involves evaluating its binding to folate receptor alpha (FRα)-expressing cancer cells and its subsequent fluorescent properties. A common protocol involves incubating FRα-positive cells, such as HeLa cells, with varying concentrations of EC-17 sodium. After incubation, the cells are washed to remove unbound compound, and the fluorescence signal is measured using a fluorescence microscope, flow cytometer, or a plate reader. The signal-to-background ratio (SBR) is calculated to determine the specificity and sensitivity of the binding. For EC-17, the SBR on HeLa cells varies from 0.97 to 7.32 depending on concentration. The spectral binding wavelength of fluorescein in EC-17 is in the range of 490-530 nm. To assess the potential for therapeutic applications, an antibody-dependent cellular cytotoxicity (ADCC) assay can be performed. In this assay, FRα-positive target cells are incubated with EC-17 sodium and then co-cultured with immune effector cells (e.g., peripheral blood mononuclear cells) in the presence of anti-fluorescein antibodies. Target cell lysis is then measured to evaluate the efficacy of ADCC. These assays are critical for characterizing the binding affinity, specificity, and functional activity of EC-17 sodium.
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| Cell Assay |
The in vitro cell-based assay for EC-17 sodium is designed to evaluate its binding to folate receptor alpha (FRα) on cancer cells and its subsequent fluorescent properties. Typically, FRα-positive cell lines such as HeLa, KB, or OVCAR-3 are cultured and then incubated with varying concentrations of EC-17 sodium. After a defined incubation period, the cells are washed to remove unbound compound, and the fluorescence signal is measured using flow cytometry or a fluorescence microscope. The concentration-dependent increase in fluorescence confirms specific binding to FRα. The signal-to-background ratio (SBR) is calculated to determine the specificity of the binding. For EC-17, the SBR on HeLa cells varies from 0.97 to 7.32 depending on concentration. To further validate the specificity, a competition assay can be performed where cells are incubated with EC-17 sodium in the presence of an excess of free folic acid, which should reduce the fluorescent signal by competing for FRα binding. Additionally, the potential for antibody-dependent cellular cytotoxicity (ADCC) can be evaluated in a cell-based assay. FRα-positive target cells are labeled with EC-17 sodium and then co-cultured with immune effector cells (e.g., NK cells) and anti-fluorescein antibodies. The degree of target cell lysis is then measured to assess the ADCC activity. These assays are essential for characterizing the compound's targeting specificity and its potential for therapeutic applications.
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| Animal Protocol |
The in vivo animal experimental protocol for EC-17 sodium typically involves the use of mouse models bearing FRα-positive tumor xenografts. To evaluate its imaging capabilities, tumor-bearing mice are injected intravenously with EC-17 sodium. After a suitable circulation time, the animals are imaged using a fluorescence imaging system to visualize the accumulation of the compound in the tumor. The fluorescence signal is quantified to assess tumor targeting and to determine the optimal time for imaging. For surgical guidance studies, mice with orthotopic or subcutaneous tumors are injected with EC-17 sodium, and then fluorescence-guided surgery is performed to resect the tumor. The efficacy of the surgery is evaluated by assessing the completeness of tumor resection and the recurrence rate. In addition to imaging, the therapeutic potential of EC-17 sodium can be evaluated in vivo. Tumor-bearing mice are treated with EC-17 sodium, sometimes in combination with anti-fluorescein antibodies, and tumor growth is monitored over time to assess the efficacy of antibody-dependent cellular cytotoxicity (ADCC). These in vivo models are essential for demonstrating the compound's utility in cancer diagnosis and therapy.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic (PK) data for EC-17 sodium, such as half-life, clearance, volume of distribution, or bioavailability, are not reported in the available literature. However, as a fluorescent contrast agent, its biodistribution and clearance are important for its in vivo performance. The compound is typically administered intravenously for imaging applications. The folate moiety of EC-17 sodium is expected to facilitate its rapid and specific binding to FRα-expressing tumors, leading to a high signal-to-background ratio in imaging studies. The FITC moiety provides the fluorescent signal for detection. The compound is likely cleared through renal and hepatic pathways, and its clearance rate would influence the optimal imaging window. The compound's stability in biological fluids and its potential for non-specific binding are also important considerations for its pharmacokinetic profile. Further studies are needed to fully characterize the PK properties of EC-17 sodium, including its absorption, distribution, metabolism, and excretion (ADME).
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| Toxicity/Toxicokinetics |
Specific toxicity (toxicology) data for EC-17 sodium are not reported in the available literature. However, as a folate conjugate, its toxicity profile is likely influenced by its targeting specificity. Since FRα is overexpressed primarily on cancer cells and has limited expression in normal tissues, EC-17 sodium is expected to have a favorable safety profile with minimal off-target effects. The compound is used for research purposes and is not intended for therapeutic use in humans. In preclinical studies, no significant toxicity has been reported at the doses used for imaging. However, comprehensive toxicological assessments, including acute and chronic toxicity studies, would be necessary to fully evaluate the safety of EC-17 sodium for potential clinical applications. The potential for immunogenicity, given the presence of the FITC moiety, and the risk of antibody-dependent cellular cytotoxicity (ADCC) in normal tissues expressing low levels of FRα would also need to be carefully assessed.
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| References | |
| Additional Infomation |
EC-17 sodium is a folate receptor alpha (FRα)-targeting fluorescent contrast agent with peak excitation and emission wavelengths of 470/520 nm. It is also known as Folate-FITC, EC17, and EC-17. The compound is a conjugate of fluorescein isothiocyanate (FITC) and folic acid, combining the targeting specificity of folate with the fluorescent properties of FITC. Its chemical formula is C42H34N10Na2O10S, and it has a molecular weight of 916.83. EC-17 sodium is used in oncology research for studying FRα expression, tumor detection, and the development of targeted imaging strategies. It offers a non-invasive and precise tool for cancer diagnostics and intraoperative guidance. In addition to its role as an imaging agent, EC-17 sodium has potential therapeutic applications through antibody-dependent cellular cytotoxicity (ADCC). The compound is available for research use only and is not for therapeutic or veterinary use. It is soluble in DMSO.
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| Molecular Formula |
C42H34N10NA2O10S
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| Molecular Weight |
916.824908733368
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| Exact Mass |
895.223
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| CAS # |
910661-33-5
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| Related CAS # |
910661-33-5 (sodium);583037-91-6 (acid);
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| Appearance |
Yellow to orange solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
591.3±50.0 °C at 760 mmHg
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| Flash Point |
311.4±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.696
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| LogP |
4.72
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| InChi Key |
BSWYZDWNAFHWBP-ARIINYJRSA-L
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| InChi Code |
InChI=1S/C42H36N10O10S.2Na/c43-41-51-36-35(38(57)52-41)48-23(19-47-36)18-46-21-3-1-20(2-4-21)37(56)50-30(40(60)61)11-12-33(55)44-13-14-45-42(63)49-22-5-8-26(29(15-22)39(58)59)34-27-9-6-24(53)16-31(27)62-32-17-25(54)7-10-28(32)34/h1-10,15-17,19,30,46,53H,11-14,18H2,(H,44,55)(H,50,56)(H,58,59)(H,60,61)(H2,45,49,63)(H3,43,47,51,52,57)/q2*+1/p-2/t30-/m0../s1
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| Chemical Name |
Benzoic acid,
5-[[[[2-[[(4S)-4-[[4-[[(2-amino-1,4-dihydro-4-oxo-6-pteridinyl)methyl]amino]benzoyl]amino]-4-carboxy-1-oxobutyl]amino]ethyl]amino]thioxomethyl]amino]-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)-,
sodium salt
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| Synonyms |
EC17 EC-17 EC 17 Folate-FTIC FTIC-Folate EC17 sodium.
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO : ~40 mg/mL (~43.63 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.6 mg/mL (1.75 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.0 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: 1.6 mg/mL (1.75 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.0 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 | 1.0907 mL | 5.4536 mL | 10.9073 mL | |
| 5 mM | 0.2181 mL | 1.0907 mL | 2.1815 mL | |
| 10 mM | 0.1091 mL | 0.5454 mL | 1.0907 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.
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