2. Protein Tyrosine Kinase/RTK
  3. Src
  4. eCF506

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.

For research use only. We do not sell to patients.

eCF506 Chemical Structure

eCF506 Chemical Structure

CAS No. : 1914078-41-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of eCF506:

eCF506 Related Antibodies

Top Publications Citing Use of Products

View All Src Isoform Specific Products:

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Lck Fyn Blk Hck Lyn Yes

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

IC50: less than 0.5 nM (Src)[1]
Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 EC50
9 nM
Compound: 11a
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
[PMID: 27115835]
In Vitro

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.

eCF506 Related Antibodies
In Vivo

eCF506 shows a moderate oral bioavailability (25.3%). A significant reduction of phospho-SRCY416 is observed in the xenograft sections from mice treated with eCF506 relative to the untreated animal controls[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

510.63

Formula

C26H38N8O3
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

NC1=C2C(C3=CC(OC)=C(NC(OC(C)(C)C)=O)C=C3)=NN(CCN4CCC(N(C)C)CC4)C2=NC=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9584 mL 9.7918 mL 19.5837 mL
5 mM 0.3917 mL 1.9584 mL 3.9167 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.77%

SDS (643 KB)

COA (251 KB) HNMR (265 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 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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eCF506 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

eCF5061914078-41-3NXP900eCF 506eCF-506NXP 900NXP-900SrcYES1/SRC inhibitoresophageal squamous cancer and breast cancerInhibitorinhibitorinhibit

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