2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Bexirestrant

Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic.

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

Bexirestrant Chemical Structure

Bexirestrant Chemical Structure

CAS No. : 2505067-70-7

Size Price Stock Quantity
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg 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.

Customer Review

Based on 1 publication(s) in Google Scholar

Bexirestrant Related Antibodies

Top Publications Citing Use of Products

View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic[1][2].

In Vitro

Bexirestrant (compound Formula Ia) inhibits the growth of wild type (WT), Y537S and D538G mutated MCF-7 cells with IC50s of 0.3. 6.0, 2.2 nM, respectively[1].
Bexirestrant induces the ER-α degradation in WT, Y537S and D538G mutated MCF-7 cells with IC50s of 0.3. 19.6, 12.7 nM, respectively[1].
Bexirestrant shows 16.3% ER-α remaining in WT MCF-7 cells at concentration of 1 nM[1].

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

Bexirestrant Related Antibodies
In Vivo

Bexirestrant (50mg/kg; p.o.; 28 days) shows a good efficacy in an MCF-Y537S xenograft[1]. Pharmacokinetic parameters in rat at 50 mg/kg p.o. dose[1]：

Tmax (h) Cmax (ng/mL) AUClast (hr× ng/mL) AUCinf_obs (hr×ng/mL) T1/2 (h)
4.00 343 7582 9804 26

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

Animal Model: Female athymic nude mice harboring subcutaneous MCF7-Y537S xenograft[1]
Dosage: 50mg/kg
Administration: p.o. for 28 days
Result: Showed 56% tumor growth inhibition compared to vehicle group after 28 days.
Molecular Weight

477.52

Formula

C29H26F3NO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(C2=CC(F)=CC(F)=C2)[C@H](C3=CC=C(C=C3)/C=C/CN4CC(C4)CF)OC5=CC(O)=CC=C51
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (209.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0942 mL 10.4708 mL 20.9415 mL
5 mM 0.4188 mL 2.0942 mL 4.1883 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0942 mL 10.4708 mL 20.9415 mL 52.3538 mL
5 mM 0.4188 mL 2.0942 mL 4.1883 mL 10.4708 mL
10 mM 0.2094 mL 1.0471 mL 2.0942 mL 5.2354 mL
15 mM 0.1396 mL 0.6981 mL 1.3961 mL 3.4903 mL
20 mM 0.1047 mL 0.5235 mL 1.0471 mL 2.6177 mL
25 mM 0.0838 mL 0.4188 mL 0.8377 mL 2.0942 mL
30 mM 0.0698 mL 0.3490 mL 0.6981 mL 1.7451 mL
40 mM 0.0524 mL 0.2618 mL 0.5235 mL 1.3088 mL
50 mM 0.0419 mL 0.2094 mL 0.4188 mL 1.0471 mL
60 mM 0.0349 mL 0.1745 mL 0.3490 mL 0.8726 mL
80 mM 0.0262 mL 0.1309 mL 0.2618 mL 0.6544 mL
100 mM 0.0209 mL 0.1047 mL 0.2094 mL 0.5235 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Bexirestrant 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:

Bexirestrant2505067-70-7Estrogen Receptor/ERRMCF-7 cellsY537S mutatD538G mutatcancerantiestrogenInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Bexirestrant
Cat. No.:
HY-145556
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (252 KB) Français - FR (252 KB) Deutsch - DE (252 KB) Norwegian - NO (252 KB) Español - ES (252 KB) Swedish - SV (252 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.