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PROTAC ERα Degrader-1

Catalog No.GC34341

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.

Products are for research use only. Not for human use. We do not sell to patients.

PROTAC ERα Degrader-1 Chemical Structure

Cas No.: 2417369-94-7

Size Price Stock Qty
5mg
$1,011.00
In stock
10mg
$1,563.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment:

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].

References:

[1]. Thomas Pillow, et al. Protac antibody conjugates and methods of use. WO2017201449A1.

Background

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.

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].

[1]. Thomas Pillow, et al. Protac antibody conjugates and methods of use. WO2017201449A1.

Chemical Properties

Cas No. 2417369-94-7 SDF
Canonical 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
Formula C66H69N7O10 M.Wt 1120.29
Solubility DMSO: 200 mg/mL (178.53 mM); Water: < 0.1 mg/mL (insoluble) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
10 mM 0.0893 mL 0.4463 mL 0.8926 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Reviews

Review for PROTAC ERα Degrader-1

Average Rating: 5 ★★★★★ (Based on Reviews and 24 reference(s) in Google Scholar.)

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