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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.

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

ErSO Chemical Structure

ErSO Chemical Structure

CAS No. : 2407860-35-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 385 In-stock
Solution
10 mM * 1 mL in DMSO USD 385 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 560 In-stock
25 mg USD 1050 In-stock
50 mg USD 1680 In-stock
100 mg USD 2650 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of ErSO:

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

a-UPR[1]

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
Molecular Weight

453.33

Formula

C22H13F6NO3

CAS No.
Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2059 mL 11.0295 mL 22.0590 mL
5 mM 0.4412 mL 2.2059 mL 4.4118 mL
View the Complete Stock Solution Preparation Table
  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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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: 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.

    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: ≥ 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.

    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: 99.75%

References

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
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ErSO 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.

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ErSO
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