E260
Based on 3 publication(s) in Google Scholar
E260 is a Fer/FerT kinase inhibitor.
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- Purity: 99.92%
- CAS No.: 1241537-79-0
- 화학식: C24H34N6S
- 분자량:438.63
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) E260
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Biological Activity
Fer/FerT kinase[1]
E260 is a Fer and FerT inhibitor, which selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level. To demonstrate that E260 directly targets Fer and FerT, an in vitro kinase assay is performed using a purified kinase domain (KD)-containing fragment of these enzymes. This analysis demonstrates the direct inhibitory effect of E260 on this domain as reflected by the significantly decreased auto-phosphorylation level of the Fer/FerT KD when incubated with ATP and increasing concentrations of E260. Moreover, computational analysis of E260 docking in the modeled whole Fer protein reveals that the highest scored binding mode of E260 to Fer falls in the ATP-binding pocket of the enzyme’s KD. To measure the dissociation constant (Kd) of E260 from Fer/FerT KD, a microscale thermophoresis (MST) test is performed using ascending concentrations of E260. This analysis corroborates the direct binding of E260 to Fer/FerT KD and determines a Kd of 0.85 μM. To examine the effect of the E260 micellar formulation on Fer in malignant cells, the kinase is immunoprecipitated from untreated and from E260-treated SW620 CC cells. When applied to metastatic grade IV SW620 CC cells, which are serum starved for 16 h and treated with 3 mM H2O2 to activate Fer, E260 exhibits inhibitory effects on the Fer-kinase activity as is reflected by suppressed auto-phosphorylation activity of the enzyme. To characterize the effect of E260 on malignant cells, metastatic SW620 cells are treated with E260 followed by analysis of viability. Onset of death is observed in the E260-treated cells, with an EC50 value of 400 nM after 24 h of treatment and an EC50 of 300 nM after 48 h. E260 exhibits an EC50 of 3.2 μM after 72 h treatment of non-metastatic PANC-1 cells, which are derived from a primary pancreatic ductal carcinoma. Moreover, the maximum death level of these cells after 72 h of treatment with E260 is about 70% following treatment with 4 μM E260. In comparison, SU.86.86 which are metastatic ductal carcinoma cells, prove to be more susceptible to E260 with an EC50 of 1.1 μM after 72 h of treatment and 100% death level imposed by 2 μM E260[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1241537-79-0
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Appearance Solid
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분자량 438.63
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화학식 C24H34N6S
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Color White to off-white
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SMILES
CC(C)C1=CC=C(C2=CN3C(SC(N4CCC(CN5CCN(C)CC5)CC4)=N3)=N2)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
Molecular landscape, subtypes, and therapeutic vulnerabilities of central nervous system solitary fibrous tumors. [Abstract]2025 Aug 23;16(1):7870. PMID: 40849425 -
Nat Commun
Spatiotemporal H2O2 flashes coordinate actin cytoskeletal remodeling and regulate cell migration and wound healing. [Abstract]2025 Jul 25;16(1):6868. PMID: 40715145 -
Biofactors
Lactate dehydrogenase A is implicated in the pathogenesis of B-cell lymphoma through regulation of the FER signaling pathway. [Abstract]2024 Sep-Oct;50(5):1024-1038. PMID: 38516823
용액&용해도
Ethanol : 10 mg/mL (22.80 mM; Need ultrasonic)
DMSO : 1 mg/mL (2.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.1 mg/mL (0.23 mM); Clear solution
This protocol yields a clear solution of ≥ 0.1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (1.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.1 mg/mL (0.23 mM); Clear solution
This protocol yields a clear solution of ≥ 0.1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (1.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 22 mg/mL (50.16 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
To test the effect of E260 on the Fer/FerT KD auto-phosphorylation activity, 0.5 µg of the Fer/FerT KD protein is incubated in 0.5 mL kinase activity buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.01% Brij-35) and 1 µM ATP. As a negative control, the KD protein is incubated in the same buffer without ATP. The KD and ATP containing mixture is incubated for 1 h at room temperature with ascending concentrations of E260 dissolved in DMSO or with DMSO alone. Following the incubation period, a sample from the incubated mixture is separated by SDS-PAGE and a WB analysis is performed using specific anti-Fer and anti-pY antibodies to evaluate the inhibitory effect of E260, as reflected by the diminished phosphorylation level of the Fer/FerT KD[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cells death level is determined using the MultiTox-Fluor Multiplex Cytotoxicity Assay. Briefly, SW620 CC cells are inoculated into black 96-well plate. After 24 h, when the cells are completely attached, 2 μM E260 or control solution are administrated at different concentrations and incubated for the desired period of time. Following the incubation period, the assay’s fluorophore which ias used to determine the cell death levels is added to each well. The relative fluorescence intensity emitted by the fluorophore from each well is determined using an ELISA reader and is compared to the florescence intensity obtained from the standard curve drawn to translate it to cell death percentage and normalized to the non-treated cells which are also used in each analysis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Nude mice are inoculated with 1.5 ×106 SW620 or SW48 CC cells and divided randomly into experimental groups. The mice are transferred from ad libitum diet to a stricter diet 2 days before inoculation to lower blood glucose levels. At this point the mice are also housed one per cage to ensure an even consumption of food. The diet is comprised of 3 g/mouse/day of standard chow, given at the same time every day. The food is consumed within an average time of 2 h, consequently the mice are kept without food for the next 22 h until the daily ration. The mice are kept on this diet throughout the experiment. The mice are randomized 4 days after tumor inoculation and placed again each in a cage. Mice are injected intraperitoneally every 12 h for 22 days with 25 or 50 mg/kg of the micellar E260 formulation, and control mice are injected with empty micelles[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Ethanol | 1 mM | 2.2798 mL | 11.3991 mL | 22.7983 mL | 56.9956 mL |
| Ethanol | 5 mM | 0.4560 mL | 2.2798 mL | 4.5597 mL | 11.3991 mL |
| 10 mM | 0.2280 mL | 1.1399 mL | 2.2798 mL | 5.6996 mL | |
| 15 mM | 0.1520 mL | 0.7599 mL | 1.5199 mL | 3.7997 mL | |
| 20 mM | 0.1140 mL | 0.5700 mL | 1.1399 mL | 2.8498 mL |
E260 Related Classifications
HY-112097 Related Classifications
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