2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. Androgen Receptor Apoptosis
  4. AR antagonist 15

AR antagonist 15 is an orally active androgen receptor (AR) antagonist with the IC50 of 97 nM for ART787A. AR antagonist 15 disrupts AR nuclear translocation, hinders AR homodimerization, and suppresses transcription of AR-regulated genes by competitive binding to the ligand binding pocket. AR antagonist 15 can significantly lower the prostate-specific antigen (PSA) level. AR antagonist 15 induces apoptosis by reducing the expression of apoptosis pathway related proteins. AR antagonist 15 can be used for the research of prostate cancer[1].

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AR antagonist 15 Chemical Structure

AR antagonist 15 Chemical Structure

CAS No. : 1790308-86-9

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AR antagonist 15 Related Antibodies

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Description

AR antagonist 15 is an orally active androgen receptor (AR) antagonist with the IC50 of 97 nM for ART787A. AR antagonist 15 disrupts AR nuclear translocation, hinders AR homodimerization, and suppresses transcription of AR-regulated genes by competitive binding to the ligand binding pocket. AR antagonist 15 can significantly lower the prostate-specific antigen (PSA) level. AR antagonist 15 induces apoptosis by reducing the expression of apoptosis pathway related proteins. AR antagonist 15 can be used for the research of prostate cancer[1].

In Vitro

AR antagonist 15 (Compound LT16) has significant antagonistic activity against androgen receptors (AR) and and its relevant mutants, including ART787A (IC50 = 97 nM), ARF877L (IC50 = 200 nM), ARF877L/T787A (IC50 = 260 nM), ARH875Y/T787A (IC50 = 200 nM), ARW742C (IC50 = 510 nM) and ART787G (IC50 = 555 nM)[1].

AR antagonist 15 reduces the prostate-specific antigen (PSA) levels secreted in a dose dependent manner with the IC50 of 0.16 μM[1].

AR antagonist 15 (48 h) impeds the translocationof AR from the cytoplasm to the nucleus[1].

AR antagonist 15 (0.1-10 μM, 48 h) can downregulate the mRNA level of AR regulated genes and significantly lowers the mRNA level of key proteins involved in the apoptosis pathway in LNCaP cells[1].

AR antagonist 15 (0.01-100 μM; 3 days or 5 days) significantly inhibits the AR positive cells proliferation[1].

AR antagonist 15 (10 μM, 48 h) induces G0/G1 cell cycle arrest in LNCaP cells[1].

AR antagonist 15 (0.5-5 μM, 14 days) inhibits the growth of LNCaP cells and reduces the number of cell colonies[1].

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

AR antagonist 15 Related Antibodies

Western Blot Analysis[1]

Cell Line: LNCaP cells
Concentration: 0.1 μM, 1 μM, 10 μM, Enzalutamide (Enz) (HY-70002) as a control group
Incubation Time: 48 h
Result: Reduced the level of protein TMPRSS2, FKBP5, and PSA.

RT-PCR[1]

Cell Line: LNCaP cells
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 48 h
Result: Reduced the mRNA level of AR regulated genes KLK3, TMPRSS2, FKBP5, c-MYC and UBE2C.
Lowed the mRNA level of proteins related to the apoptosis pathway Cyclin A, CDK1, CDC20, and CKS2.

Cell Viability Assay[1]

Cell Line: LNCaP, LNCaP-CRPC, LNCaP-EnzR, VCaP, 22Rv1, and C4-2B cells
Concentration: 5 days for LNCaP and LNCaP-CRPC cells; 3 days for LNCaP-EnzR, VCaP, 22Rv1, and C4-2B cells
Incubation Time: 48 h
Result: Exhibited a relatively better antiproliferative effect in LNCaP (IC50 = 5.31 μM), LNCaP-CRPC (IC50 = 8.05 μM) and LNCaP-EnzR (IC50 = 5.40 μM).

Cell Cycle Analysis[1]

Cell Line: LNCaP cells
Concentration: 10 μM
Incubation Time: 48 h
Result: Caused cell cycle arrest in G0/G1.

Cell Proliferation Assay[1]

Cell Line: LNCaP cells
Concentration: 0.5 μM, 10 μM
Incubation Time: 14 days
Result: Significantly inhibited the number of cell colonies.
In Vivo

AR antagonist 15 (50 mg/kg; i.g.; once daily; for three weeks) significantly reduces tumor volume and decreases serum the PSA level in the Balb/C nude male prostate cancer mice[1].

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

Animal Model: 1×107 LNCaP cells injected the Balb/C nude male mice (4-6 weeks)[1]
Dosage: 50 mg/kg
Administration: Oral gavage (i.g.); once daily for three weeks
Result: Significantly reduced tumor volume and tumor weight of the cancer mice and the final tumor growth inhibition (TGI) rate was 75.63%.
Significantly inhibited the PSA level and the concentration of the PSA droped to 11.08 ng/mL. Did not cause significant changes in the weight of the mice.
Molecular Weight

346.44

Formula

C18H22N2O3S
CAS No.
SMILES

O=S(NC1=CC=C(C=C1)OCC2=CC=CC=C2)(N3CCCCC3)=O
Shipping

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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References
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AR antagonist 15 Related Classifications

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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.

Keywords:

AR antagonist 151790308-86-9AR antagonist15AR antagonist-15Androgen ReceptorApoptosisprostate canceranticancerPSAapoptosisInhibitorinhibitorinhibit

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