EC17 sodium (Folate-FITC) is a fluorescein isothiocyanate (FITC) conjugated folic acid with potential antineoplastic activity. It also acts as a FRα-targeting agent that fluoresces at 500nm. EC17 is conjugate consisting of fluorescein isothiocyanate (FITC) conjugated with folate with potential antineoplastic activity. Folate-FITC binds to folate receptors, which are overexpressed on the surfaces of many cancer cells including kidney and ovarian cancer cells. Once bound to the cancer cell through the folate moiety of the conjugate, curculating anti-fluorescein antibodies.may recognize and bind to the FITC moiety, resulting in antibody-dependent cellular cytotoxicity.
Physicochemical Properties
| Molecular Formula | C42H34N10NA2O10S |
| Molecular Weight | 916.824908733368 |
| Exact Mass | 895.223 |
| CAS # | 910661-33-5 |
| Related CAS # | 910661-33-5 (sodium);583037-91-6 (acid); |
| Appearance | Yellow to orange solid powder |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 591.3±50.0 °C at 760 mmHg |
| Flash Point | 311.4±30.1 °C |
| Vapour Pressure | 0.0±1.7 mmHg at 25°C |
| Index of Refraction | 1.696 |
| LogP | 4.72 |
| InChi Key | BSWYZDWNAFHWBP-ARIINYJRSA-L |
| 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 |
| 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 |
| Synonyms | EC17 EC-17 EC 17 Folate-FTIC FTIC-Folate EC17 sodium. |
| 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: 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) |
Biological Activity
| 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]. |
| 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]. |
| References |
[1]. Intraoperative imaging of folate receptor alpha positive ovarian and breast cancer using the tumor specific agent EC17. Oncotarget. 2016 May 31;7(22):32144-55. |
Solubility Data
| Solubility (In Vitro) |
DMSO : ~40 mg/mL (~43.63 mM) H2O : < 0.1 mg/mL |
| 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 |