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    Ligand for Target Protein for PROTAC
  3. Androgen receptor antagonist 1

Androgen receptor antagonist 1 

Cat. No.: HY-130992
Handling Instructions

Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

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

Androgen receptor antagonist 1 Chemical Structure

Androgen receptor antagonist 1 Chemical Structure

CAS No. : 1338812-36-4

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Description

Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM[1]. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively[2].

IC50 & Target

IC50: 59 nM (androgen receptor)[1]

In Vitro

Androgen receptor antagonist 1 (Compound 26; 1 nM-100 μM) shows significant cell growth inhibition effects for LNCaP and LNAR cells but not DU145 cells[1].

Cell Proliferation Assay[1]

Cell Line: Prostate cancer (CaP) cells (LNCAP, LNAR, and DU145)
Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM
Incubation Time: 7 days
Result: Antiproliferative effects of in LNCAP and LNAR cells.
In Vivo

Androgen receptor antagonist 1 (Compound 26; 100 mg/kg once a day for 5 weeks) demonstrates excellent in vivo tumor growth inhibition upon oral administration in a castration-resistant prostate cancer (CRPC) animal model[1].

Animal Model: Male athymic nude mice with LNCaP xenograft model of CRPC[1]
Dosage: 100 mg/kg
Administration: Orally once a day for 5 weeks
Result: Demonstrated outstanding efficacy in inhibiting tumor growth. At the given doses (100 mg/kg once a day) nearly completely suppressed tumor growth (by 90 %) and the PSA levels (78%) after 5 weeks, with no detectable body weight loss for the period of time when animals were treated.
Molecular Weight

416.90

Formula

C₂₁H₂₅ClN₄O₃

CAS No.

1338812-36-4

SMILES

O=C(C1=CN(CCO)N=C1)N[[email protected]]2C(C)(C)[[email protected]](OC3=CC=C(C#N)C(Cl)=C3)C2(C)C

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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:

Androgen receptor antagonist 1Androgen receptor antagonist1Androgen receptor antagonist-1Androgen ReceptorLigand for Target Protein for PROTACTarget Protein-binding MoietyandrogenreceptorPROTAC LNCaPtumorcastrationresistantprostatecancerCRPCInhibitorinhibitorinhibit

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Androgen receptor antagonist 1
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HY-130992
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