1. PROTAC Vitamin D Related/Nuclear Receptor
  2. PROTACs Estrogen Receptor/ERR
  3. PROTAC ERα Degrader-1

PROTAC ERα Degrader-1 

Cat. No.: HY-112098 Purity: 99.59% ee.: 98.35%
COA Handling Instructions

PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.

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

PROTAC ERα Degrader-1 Chemical Structure

PROTAC ERα Degrader-1 Chemical Structure

CAS No. : 2417369-94-7

Size Price Stock Quantity
2 mg USD 850 In-stock
5 mg USD 1500 In-stock
10 mg USD 2300 In-stock
25 mg USD 4100 In-stock
50 mg USD 6200 In-stock
100 mg   Get quote  
200 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

Other Forms of PROTAC ERα Degrader-1:

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Estrogen Receptor/ERR Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.

IC50 & Target

Estrogen receptor-alpha (ERα)[1]

In Vitro

Treatment of the HER2 expressing cells with the PROTAC ERα Degrader-1 (without Ab; compound P1) results in a decreased estrogen receptor-alpha (ERα) levels[1].

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

Molecular Weight

1120.29

Formula

C66H69N7O10

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

OC1=CC=C(/C(C2=CC=C(OCCN(C)C(COCCOCCNC(C3=CC=C(C(N4[C@@H](C)[C@H](NC([C@H](C)NC)=O)C(N(CC5=C(OC)C=CC6=C5C=CC=C6)C7=C4C=C(C#N)C=C7)=O)=O)C=C3)=O)=O)C=C2)=C(C8=CC=CC=C8)\CC)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (178.53 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 0.8926 mL 4.4631 mL 8.9263 mL
5 mM 0.1785 mL 0.8926 mL 1.7853 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 (stored under nitrogen). 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:

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    90% (20% SBE-β-CD in Saline)

    Solubility: 5 mg/mL (4.46 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5 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 (50.0 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.
  • Protocol 2

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

    Solubility: ≥ 5 mg/mL (4.46 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

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

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: 99.59% ee.: 98.35%

References
Kinase Assay
[1]

Synthesis of a PROTAC:
i. Attachment of a Linker (L2) to an E3 Ligase Binding Group (E3LB).
ii. Attachment of a protein binding moiety (PB) to an E3LB via a Linker (L2)[1].

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

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 (stored under nitrogen). 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 0.8926 mL 4.4631 mL 8.9263 mL 22.3156 mL
5 mM 0.1785 mL 0.8926 mL 1.7853 mL 4.4631 mL
10 mM 0.0893 mL 0.4463 mL 0.8926 mL 2.2316 mL
15 mM 0.0595 mL 0.2975 mL 0.5951 mL 1.4877 mL
20 mM 0.0446 mL 0.2232 mL 0.4463 mL 1.1158 mL
25 mM 0.0357 mL 0.1785 mL 0.3571 mL 0.8926 mL
30 mM 0.0298 mL 0.1488 mL 0.2975 mL 0.7439 mL
40 mM 0.0223 mL 0.1116 mL 0.2232 mL 0.5579 mL
50 mM 0.0179 mL 0.0893 mL 0.1785 mL 0.4463 mL
60 mM 0.0149 mL 0.0744 mL 0.1488 mL 0.3719 mL
80 mM 0.0112 mL 0.0558 mL 0.1116 mL 0.2789 mL
100 mM 0.0089 mL 0.0446 mL 0.0893 mL 0.2232 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.

PROTAC ERα Degrader-1 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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PROTAC ERα Degrader-1
Cat. No.:
HY-112098
Quantity:
MCE Japan Authorized Agent: