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  3. ERα degrader-2

ERα degrader-2 

Cat. No.: HY-132194
Handling Instructions

ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent druggability, can be used for HER+ breast cancer research.

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

ERα degrader-2 Chemical Structure

ERα degrader-2 Chemical Structure

CAS No. : 2235396-63-9

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Description

ERα degrader-2 is a selective estrogen receptor degrader (SERD) with potent binding affinity with ERα (IC50=17.1 nM), good degradation efficacy (EC50=0.3 nM). ERα degrader-2 exhibits favorable pharmacokinetic properties and excellent druggability, can be used for HER+ breast cancer research[1].

IC50 & Target[1]

ERα

4.6 nM (IC50)

In Vitro

ERα degrader-2 (0.01-40 nM) decreases ERα expression and not fully degrades ERα in MCF-7 cells even at a higher biochemical concentration in MCF7 cells[1].

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

In Vivo

ERα degrader-2 (oral administration; 2-6 mg/kg; QD; 21 days) leads to the significant tumor growth inhibition and decreases tumor volume in mice[1].
ERα degrader-2 (oral gavage; 2 mg/kg; single dose) possesses better pharmacokinetic properties than AZD9496, the plasma exposure (AUC) is 16073.7 h*ng/mL, and the half-life period is 12.1 h, the oral availability is 80.5%[1].

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

Animal Model: MCF-7 human breast cancer xenograft model in nude mice[1]
Dosage: 2 mg/kg; 6 mg/kg
Administration: Oral administration; 2-6 mg/kg; QD; 21 days
Result: Exhibited in vivo efficacy in breast cancer xenograft model.
Molecular Weight

492.53

Formula

C₂₉H₂₇F₃N₂O₂

CAS No.
SMILES

CC(C)(F)CN1[[email protected]@](C2=C(C=C(C3=CC=C(C=C3)C(O)=O)C=C2F)F)([H])C4=C(C[[email protected]]1C)C5=CC=CC=C5N4

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

ERα degrader-2ERα degrader2ERα degrader 2Estrogen Receptor/ERRSERDdegradeMCF-7breast cancerERαHER2+Inhibitorinhibitorinhibit

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ERα degrader-2
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HY-132194
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