Art. -Nr.: HY-132247

ErSO

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ErSO is a selective anticipatory unfolded protein response (a-UPR) activator. ErSO acts through ERα to elicit strong and sustained cytotoxic activation of the a-UPR. ErSO can be used for the research of cancer.

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Reinheit: 99.95%
CAS. Nr.: 2407860-35-7
Formel: C₂₂H₁₃F₆NO₃
Molecular Weight:453.33

Speicherung:

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

ErSO Chemical Structure

CAS. Nr.: 2407860-35-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

a-UPR^[1]

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	12.4 μM Compound: ErSO	Anticancer activity against mouse 4T1 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against mouse 4T1 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
A549	IC₅₀	12.4 μM Compound: ErSO	Anticancer activity against human A549 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human A549 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
BT-20	IC₅₀	34 nM Compound: ErSO	Anticancer activity against human BT-20 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human BT-20 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
BT-474	IC₅₀	34 nM Compound: ErSO	Anticancer activity against human BT-474 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human BT-474 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
BT-549	IC₅₀	12.4 μM Compound: ErSO	Anticancer activity against human BT-549 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human BT-549 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
Caov-3 cell line	IC₅₀	34 nM Compound: ErSO	Anticancer activity against human Caov-3 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human Caov-3 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
HCC1806	IC₅₀	12.4 μM Compound: ErSO	Anticancer activity against human HCC1806 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human HCC1806 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
HCT-116	IC₅₀	12.4 μM Compound: ErSO	Anticancer activity against human HCT-116 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human HCT-116 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
HepG2	IC₅₀	12.4 μM Compound: ErSO	Anticancer activity against human HepG2 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human HepG2 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
HL-60	IC₅₀	34 nM Compound: ErSO	Anticancer activity against human HL-60 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human HL-60 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
HOS	IC₅₀	12.4 μM Compound: ErSO	Anticancer activity against human HOS cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human HOS cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
Hs-578T	IC₅₀	34 nM Compound: ErSO	Anticancer activity against human Hs-578T cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human Hs-578T cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
IGROV-1	IC₅₀	12.4 μM Compound: ErSO	Anticancer activity against human IGROV-1 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human IGROV-1 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
K562	IC₅₀	12.4 μM Compound: ErSO	Anticancer activity against human K562 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human K562 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
MCF7	IC₅₀	34 nM Compound: ErSO	Anticancer activity against human MCF7 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human MCF7 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
MDA-MB-231	IC₅₀	12.4 μM Compound: ErSO	Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
MDA-MB-436	IC₅₀	12.4 μM Compound: ErSO	Anticancer activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human MDA-MB-436 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
MDA-MB-453	IC₅₀	34 nM Compound: ErSO	Anticancer activity against human MDA-MB-453 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human MDA-MB-453 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
MDA-MB-468	IC₅₀	34 nM Compound: ErSO	Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
OVCAR-3	IC₅₀	34 nM Compound: ErSO	Anticancer activity against human OVCAR-3 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human OVCAR-3 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
PC-3	IC₅₀	34 nM Compound: ErSO	Anticancer activity against human PC-3 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human PC-3 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
T47D	IC₅₀	34 nM Compound: ErSO	Anticancer activity against human T47D cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human T47D cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]
ZR-75-1	IC₅₀	34 nM Compound: ErSO	Anticancer activity against human ZR-75-1 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human ZR-75-1 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35814932]

In Vitro

ErSO (1~1000 nM; 24 hours; MCF-7 cells) shows that IC₅₀ value is 20.3 nM in MCF-7 cells and inhibits cell viability^[1].
ErSO (1 μM; 24 hours; TYS cells) rapidly kills ERα-positive breast cancer cells. ErSO is effective against both the breast cancer cell lines expressing wild-type ERα and the ERαY537S and ERαD538G mutations such as human breast cancer cell lines TYS and TDG. ErSO is also effective against tamoxifen- and fulvestrant-resistant breast cancer cell lines containing wild-type ERα. ErSO activity is independent of the presence of estrogen. ErSO induces rapid killing of ERα-positive MCF-7 human breast cancer cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

MCF-7 cells
Concentration:

1~1000 nM
Incubation Time:

24 hours
Result:

Showed that IC₅₀ value is 20.3 nM in MCF-7 cells and inhibited cell viability.

In Vivo

ErSO (10 or 40 mg/kg; p.o.; 21 days) results in elimination of these tumors, with >90% reduction in all cases^[1].
ErSO (0.5~40 mg/kg; p.o.; 3 weeks) is sufficient for a robust response^[1].
ErSO (10 and 40 mg/kg; p.o.; 14 days) induces >10,000-fold regression of TYS-luciferase-expressing breast tumors in all five mice and >100,000-fold regression (to undetectable amounts) within 14 days as shown by bioluminescent imaging of luciferase as compared to vehicle-treated mice^[1].
ErSO (40 mg/kg; i.p.; 14 days) greatly reduces metastatic burden^[1].
ErSO treatment ablates mutant ERα breast cancer cell line xenografts and a PDX mouse model^[1].

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

Animal Model:

Nu/J mice^[1]
Dosage:

10 or 40 mg/kg
Administration:

P.o.; 21 days
Result:

Resulted in elimination of these tumors, with >90% reduction in all cases.

Animal Model:

Mice^[1]
Dosage:

0.5~40 mg/kg
Administration:

P.o.; 3 weeks
Result:

Sufficient for a robust response.

Animal Model:

Mice^[1]
Dosage:

40 mg/kg
Administration:

I.p.; 14 days
Result:

Metastatic burden was greatly reduced

Chemical Information

CAS. Nr. 2407860-35-7
Appearance Solid
Molecular Weight 453.33
Formel C₂₂H₁₃F₆NO₃
Color White to off-white
SMILES

O=C1NC2=C(C=CC=C2C(F)(F)F)[C@@]1(C3=CC=C(O)C=C3)C4=CC=C(OC(F)(F)F)C=C4
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 : 120 mg/mL (264.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.2059 mL

11.0295 mL

22.0590 mL

5 mM

0.4412 mL

2.2059 mL

4.4118 mL

10 mM

0.2206 mL

1.1029 mL

2.2059 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: 5.25 mg/mL (11.58 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 5.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (52.5 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: ≥ 3 mg/mL (6.62 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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: ≥ 3 mg/mL (6.62 mM); Clear solution

This protocol yields a clear solution of ≥ 3 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 (30.0 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 (281 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]. Boudreau MW, et al. A small-molecule activator of the unfolded protein response eradicates human breast tumors in mice. Sci Transl Med. 2021;13(603):eabf1383. [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	2.2059 mL	11.0295 mL	22.0590 mL	55.1475 mL
	5 mM	0.4412 mL	2.2059 mL	4.4118 mL	11.0295 mL
	10 mM	0.2206 mL	1.1029 mL	2.2059 mL	5.5147 mL
	15 mM	0.1471 mL	0.7353 mL	1.4706 mL	3.6765 mL
	20 mM	0.1103 mL	0.5515 mL	1.1029 mL	2.7574 mL
	25 mM	0.0882 mL	0.4412 mL	0.8824 mL	2.2059 mL
	30 mM	0.0735 mL	0.3676 mL	0.7353 mL	1.8382 mL
	40 mM	0.0551 mL	0.2757 mL	0.5515 mL	1.3787 mL
	50 mM	0.0441 mL	0.2206 mL	0.4412 mL	1.1029 mL
	60 mM	0.0368 mL	0.1838 mL	0.3676 mL	0.9191 mL
	80 mM	0.0276 mL	0.1379 mL	0.2757 mL	0.6893 mL
	100 mM	0.0221 mL	0.1103 mL	0.2206 mL	0.5515 mL

Keywords

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ErSO

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators 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

Anti-Cancer Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Activators 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 Related Classifications

HY-132247 Related Classifications