eCF506
Based on 7 publication(s) in Google Scholar
eCF506 (NXP900) is a highly potent and orally active YES1/SRC kinase inhibitor with an IC50 of 0.47 nM. eCF506 locks its target into its native “closed” conformation, thereby inhibiting both kinase activity and complex formation with protein partners. eCF506 can be used for the study of esophageal squamous cancer and breast cancer.
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- Pureté: 99.09%
- CAS No.: 1914078-41-3
- Formule: C26H38N8O3
- Masse moléculaire:510.63
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) eCF506
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Activité biologique
IC50: less than 0.5 nM (Src)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | EC50 |
9 nM
Compound: 11a
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Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 5 days by PrestoBlue assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 5 days by PrestoBlue assay
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[PMID: 27115835] |
eCF506 induces a very potent antiproliferative effect in both MCF7 and MDA-MB-231 cells. eCF506 inhibits phosphorylation of SRC and FAK at low nanomolar levels, with complete inhibition observed at 100 nM. eCF506 significantly reduces cell motility at 10 nM as early as 6 h into the study, with equivalent efficacy to dasatinib. eCF506 exclusively inhibits SFK, with subnanomolar IC50 values against SRC and YES (IC50=0.5, 2.1 nM). It is important to highlight that eCF506 displays a vast difference in activity (>950-fold difference) between ABL and its primary target SRC[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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1914078-41-3
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Appearance Solid
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Masse moléculaire 510.63
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Formule C26H38N8O3
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Color White to yellow
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SMILES
NC1=C2C(C3=CC(OC)=C(NC(OC(C)(C)C)=O)C=C3)=NN(CCN4CCC(N(C)C)CC4)C2=NC=N1
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Synonyms
NXP900
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
J Clin Invest
Coordinated activation of c-Src and FOXM1 drives tumor cell proliferation and breast cancer progression. [Abstract]2023 Apr 3;133(7):e162324. PMID: 36795481 -
J Med Chem
2024 Nov 28;67(22):20571-20579. PMID: 39513680 -
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Solvant et solubilité
DMSO : 62.5 mg/mL (122.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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: ≥ 2.08 mg/mL (4.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 50% PEG300 50% Saline
Solubility: 2.5 mg/mL (4.90 mM); Clear 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.
Protocole
MDA-MB-231 cells are treated with eCF506 or dasatinib (10 nM), and cell migration compared with untreated cell control (DMSO, 0.1%, v/v) at 6, 12, and 24 h. Cells are imaged and analyzed using an IncuCyte-ZOOM microscope with integrated scratch-wound migration software module[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
In vivo PD study is performed in a xenograft model of HCT116 cells in mice. HCT116 cells are injected subcutaneously, and tumors are allowed to grow up to 3-mm in diameter. Subsequently, mice are dosed daily for 3 d with eCF506 (50 mg/kg, in nanopure water) or vehicle (nanopure water) by oral gavage and culled 3 h after the last dose (n=4). Tumors are excised, fixed, and sections labeled for phospho-SRCY416 and stained with hematoxylin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (280 KB)
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SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Portuguese - PT (644 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 1 mM | 1.9584 mL | 9.7918 mL | 19.5837 mL | 48.9591 mL |
| 5 mM | 0.3917 mL | 1.9584 mL | 3.9167 mL | 9.7918 mL | |
| 10 mM | 0.1958 mL | 0.9792 mL | 1.9584 mL | 4.8959 mL | |
| 15 mM | 0.1306 mL | 0.6528 mL | 1.3056 mL | 3.2639 mL | |
| 20 mM | 0.0979 mL | 0.4896 mL | 0.9792 mL | 2.4480 mL | |
| 25 mM | 0.0783 mL | 0.3917 mL | 0.7833 mL | 1.9584 mL | |
| 30 mM | 0.0653 mL | 0.3264 mL | 0.6528 mL | 1.6320 mL | |
| 40 mM | 0.0490 mL | 0.2448 mL | 0.4896 mL | 1.2240 mL | |
| 50 mM | 0.0392 mL | 0.1958 mL | 0.3917 mL | 0.9792 mL | |
| 60 mM | 0.0326 mL | 0.1632 mL | 0.3264 mL | 0.8160 mL | |
| 80 mM | 0.0245 mL | 0.1224 mL | 0.2448 mL | 0.6120 mL | |
| 100 mM | 0.0196 mL | 0.0979 mL | 0.1958 mL | 0.4896 mL |
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