eCF506

Name: eCF506
Brand: MedChemExpress
SKU: HY-112096
Rating: 4.5 (2 reviews)

Cat. No.: HY-112096 Purity: 99.30%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 1914078-41-3

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 124	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 124	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 52	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 275	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 715	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE eCF506

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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].

MedChemExpress (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-SRC^Y416 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.

1914078-41-3

Appearance

Solid

Color

Light yellow 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
10 mM	0.1958 mL	0.9792 mL	1.9584 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.30%

Select Batch:

Data Sheet (277 KB) SDS (0 KB)

COA (251 KB) LCMS (270 KB)

Handling Instructions (2659 KB)

References

[1]. Fraser C, et al. Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. J Med Chem. 2016 May 26;59(10):4697-710. [Content Brief]

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	[1]. Fraser C, et al. Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. J Med Chem. 2016 May 26;59(10):4697-710. [Content Brief]

Complete Stock Solution Preparation Table

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

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:

eCF5061914078-41-3eCF 506eCF-506SrcInhibitorinhibitorinhibit

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eCF506

Customer Review

eCF506 Related Antibodies

2 Publications Citing Use of MCE eCF506

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Src Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

eCF506 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

eCF506 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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