Art. -Nr.: HY-144070

ErSO-DFP

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ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator. ErSO-DFP has enhanced selectivity for estrogen receptor alpha-positive (ERα+) cancer cells with a wider selectivity window than ErSO (HY-132247). ErSO-DFP displays antitumor activity against MCF-7 in mice. ErSO-DFP can cross the blood brain barrier.

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Reinheit: 99.56%
CAS. Nr.: 2768139-76-8
Formel: C₂₀H₁₇F₅N₂O₂
Molecular Weight:412.35

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

ErSO-DFP Chemical Structure

CAS. Nr.: 2768139-76-8

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

In Vitro

ErSO-DFP (0-100 μM, 24-72 h) exhibits cytotoxicity in ERα-positive cells, IC₅₀s for MCF-7, T47D, TYS and TDG are 17 nM, 16 nM, 7 nM and 9 nM, respectively^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

MCF-7, T47D, TYS and TDG
Concentration:

0-100 μM
Incubation Time:

24-72 h
Result:

Induced cell death.

In Vivo

ErSO-DFP (5 mg/kg, iv, once weekly for 3 doses) exhibits antitumor activity in MCF-7 xenograft mouse models without significant toxicity^[1].

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

Animal Model:

MCF-7 xenograft mouse models^[1]
Dosage:

5 mg/kg
Administration:

iv, once weekly for 3 doses
Result:

Inhibited the tumor growth, decreased the tumor volume, and caused no weight loss.

Chemical Information

CAS. Nr. 2768139-76-8
Appearance Solid
Molecular Weight 412.35
Formel C₂₀H₁₇F₅N₂O₂
Color White to pink
SMILES

O=C1NC2=C(C=CC=C2[C@]1(N3CCC(F)(CC3)F)C4=CC=C(C=C4)O)C(F)(F)F
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (242.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4251 mL

12.1256 mL

24.2512 mL

5 mM

0.4850 mL

2.4251 mL

4.8502 mL

10 mM

0.2425 mL

1.2126 mL

2.4251 mL

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 5 mg/mL (12.13 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (12.13 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (12.13 mM); Clear solution

This protocol yields a clear solution of ≥ 5 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Matthew W Boudreau, et al. Activators of the Anticipatory Unfolded Protein Response with Enhanced Selectivity for Estrogen Receptor Positive Breast Cancer. J Med Chem. 2022 Mar 10;65(5):3894-3912. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4251 mL	12.1256 mL	24.2512 mL	60.6281 mL
	5 mM	0.4850 mL	2.4251 mL	4.8502 mL	12.1256 mL
	10 mM	0.2425 mL	1.2126 mL	2.4251 mL	6.0628 mL
	15 mM	0.1617 mL	0.8084 mL	1.6167 mL	4.0419 mL
	20 mM	0.1213 mL	0.6063 mL	1.2126 mL	3.0314 mL
	25 mM	0.0970 mL	0.4850 mL	0.9700 mL	2.4251 mL
	30 mM	0.0808 mL	0.4042 mL	0.8084 mL	2.0209 mL
	40 mM	0.0606 mL	0.3031 mL	0.6063 mL	1.5157 mL
	50 mM	0.0485 mL	0.2425 mL	0.4850 mL	1.2126 mL
	60 mM	0.0404 mL	0.2021 mL	0.4042 mL	1.0105 mL
	80 mM	0.0303 mL	0.1516 mL	0.3031 mL	0.7579 mL
	100 mM	0.0243 mL	0.1213 mL	0.2425 mL	0.6063 mL

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ErSO-DFP

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ErSO-DFP

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ErSO-DFP Related Classifications

HY-144070 Related Classifications