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

eCF506 

Cat. No.: HY-112096 Purity: 99.30%
COA Handling Instructions

eCF506 is a highly potent and orally bioavailable inhibitor of the non-receptor tyrosine kinase Src with an IC50 of less than 0.5 nM.

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
Solution
10 mM * 1 mL in DMSO USD 123 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 123 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 165 In-stock
25 mg USD 275 In-stock
50 mg USD 495 In-stock
100 mg USD 715 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

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Based on 2 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

eCF506 is a highly potent and orally bioavailable inhibitor of the non-receptor tyrosine kinase Src with an IC50 of less than 0.5 nM.

IC50 & Target

IC50: less than 0.5 nM (Src)[1]
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].

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

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

510.63

Appearance

Solid

Formula

C26H38N8O3
CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (122.40 mM; Need ultrasonic)

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
10 mM 0.1958 mL 0.9792 mL 1.9584 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.30%

COA (251 KB) LCMS (270 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
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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.

  • Molarity Calculator

  • Dilution Calculator

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

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

eCF5061914078-41-3eCF 506eCF-506SrcInhibitorinhibitorinhibit

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