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  3. PROTAC ERα Degrader-1

PROTAC ERα Degrader-1 

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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 3081 In-stock
Estimated Time of Arrival: December 31
2 mg USD 850 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
10 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

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Based on 1 publication(s) in Google Scholar

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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].

Molecular Weight

1120.29

Formula

C₆₆H₆₉N₇O₁₀

SMILES

OC1=CC=C(/C(C2=CC=C(OCCN(C)C(COCCOCCNC(C3=CC=C(C(N4[[email protected]@H](C)[[email protected]](NC([[email protected]](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)

H2O : < 0.1 mg/mL (insoluble)

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
10 mM 0.0893 mL 0.4463 mL 0.8926 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (4.46 mM); Clear solution

*All of the co-solvents are provided by MCE.
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
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Keywords:

PROTAC ERα Degrader-1PROTAC ERα Degrader1PROTAC ERα Degrader 1PROTACEstrogen Receptor/ERRProteolysis-targeting chimeraInhibitorinhibitorinhibit

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Product name:
PROTAC ERα Degrader-1
Cat. No.:
HY-112098
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