2. Vitamin D Related/Nuclear Receptor Immunology/Inflammation
  3. Androgen Receptor Kallikrein
  4. JNJ-pan-AR

JNJ-pan-AR is an orally active androgen receptor (AR) inhibitor with an IC50 of 19 nM and a Ki of 8.4 nM against human wild-type AR. JNJ-pan-AR abolishes androgen-induced KLK2 and KLK3 mRNA expression and reduces androgen-dependent colony formation in prostate cancer cells. JNJ-pan-AR blocks AR nuclear translocation, inhibits PSA protein expression, and represses the growth of AR-dependent tumor cells and ARF877L-driven tumor xenografts. JNJ-pan-AR blocks transactivation and signaling of wild-type AR and various mutant AR variants. JNJ-pan-AR is applicable for research on castration-resistant prostate cancer.

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JNJ-pan-AR

JNJ-pan-AR Chemical Structure

CAS No. : 1332390-06-3

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JNJ-pan-AR Related Antibodies

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Description

JNJ-pan-AR is an orally active androgen receptor (AR) inhibitor with an IC50 of 19 nM and a Ki of 8.4 nM against human wild-type AR. JNJ-pan-AR abolishes androgen-induced KLK2 and KLK3 mRNA expression and reduces androgen-dependent colony formation in prostate cancer cells. JNJ-pan-AR blocks AR nuclear translocation, inhibits PSA protein expression, and represses the growth of AR-dependent tumor cells and ARF877L-driven tumor xenografts. JNJ-pan-AR blocks transactivation and signaling of wild-type AR and various mutant AR variants. JNJ-pan-AR is applicable for research on castration-resistant prostate cancer[1][2].

In Vitro

JNJ-pan-AR (compound 4) potently and selectively binds to wild-type androgen receptor with an IC50 of 19 nM and a Ki of 8.4 nM, and has minimal affinity for glucocorticoid receptor[1].
JNJ-pan-AR acts as a full antagonist of F877L mutant androgen receptor in HepG2 cells transiently transfected with VP16-AR F877L, with an IC50 of 127 nM[1].
JNJ-pan-AR acts as a full antagonist of wild-type androgen receptor in HepG2 cells transiently transfected with VP16-AR, with no agonist activity observed[1].
JNJ-pan-AR fully antagonizes wild-type androgen receptor-mediated transcriptional activity in LNCaP AR cs cells with an IC50 of 191 nM, with no agonist activity[1].
JNJ-pan-AR fully antagonizes F877L mutant androgen receptor-mediated transcriptional activity in LNCaP F877L cells with an IC50 of 98 nM, with no agonist activity[1].
JNJ-pan-AR inhibits androgen-dependent proliferation of VCaP prostate cancer cells (wild-type AR) with an IC50 of 92 nM[1].
JNJ-pan-AR effectively antagonizes transcriptional activity of androgen receptor ligand binding domain mutants (L702H, T878A, W742C, W875L) in transiently transfected HepG2 cells[1].
JNJ-pan-AR potently blocks nuclear translocation of ARF877L mutant androgen receptor and inhibits PSA expression in LNCaP F877L cells, regardless of androgen stimulation[1].
JNJ-pan-AR inhibits androgen-stimulated nuclear translocation of wild-type androgen receptor in LNCaP cells[1].
JNJ-pan-AR (0.01-10 μM; 24 h) potently inhibits androgen-mediated KLK2 and KLK3 mRNA expression in LNCaP prostate cancer cells[2].
JNJ-pan-AR (0.062-1 μM; 14 day) inhibits androgen-driven colony formation in LNCaP prostate cancer cells[2].
JNJ-pan-AR (10 μM; >3 months chronic exposure, continuous maintenance) generates LNCaP JNJR prostate cancer cells with acquired resistance to JNJ-pan-AR, characterized by altered morphology and reduced growth rate[2].
JNJ-pan-AR (0.1-10 μM; 14 day) shows that exogenous AKR1C3 expression induces partial resistance to JNJ-pan-AR in LNCaP prostate cancer cells[2].

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

JNJ-pan-AR Related Antibodies

Real Time qPCR[2]

Cell Line: LNCaP (AR-mutant T877A) prostate cancer cells
Concentration: 0.01 μM, 0.1 μM, 1 μM, 10 μM
Incubation Time: 24 h
Result: Suppressed androgen-mediated induction of KLK2 and KLK3 mRNA expression in a concentration-dependent manner.
Reduced KLK2 mRNA fold change to ~15 (from ~50 with DMSO + R1881) at 10 μM.
Reduced KLK3 mRNA fold change to ~6 (from ~14 with DMSO + R1881) at 10 μM.

Cell Proliferation Assay[2]

Cell Line: LNCaP (AR-mutant T877A) prostate cancer cells
Concentration: 0.062 μM, 0.125 μM, 0.250 μM, 0.500 μM, 1 μM
Incubation Time: 14 day
Result: Inhibited androgen-mediated colony formation efficiency in a concentration-dependent manner.
Reduced relative colony number to near baseline levels (comparable to cells treated with DMSO without R1881) at 1 μM.

Cell Proliferation Assay[2]

Cell Line: AKR1C3-overexpressing LNCaP (LNCaP AKR1C3) prostate cancer cells, vector control LNCaP Puro cells
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 14 day
Result: Resulted in significantly higher colony formation efficiency in LNCaP AKR1C3 cells than LNCaP Puro cells at all tested concentrations.
Achieved a relative colony number (normalized to DMSO) of ~0.45 for LNCaP AKR1C3 cells at 0.1 μM.
Achieved a relative colony number (normalized to DMSO) of ~0.4 for LNCaP AKR1C3 cells at 10 μM.
Parmacokinetics
Species Dose Route AUClast Cmax F CL T1/2 Vdss
Mice[1] 10 mg/kg p.o. 9.4 μg·h/mL 0.98 μM 56 % / / /
Mice[1] 2 mg/kg i.v. / / / 4.12 mL/min/kg 46.4 h 12.0 L/kg
In Vivo

JNJ-pan-AR (compound 4) (10-30 mg/kg; p.o.; daily) produces dose-dependent tumor growth inhibition in Enzalutamide (HY-70002)-resistant castration-resistant prostate cancer xenografts, with complete growth stasis (100.8% TGI) at a 30 mg/kg daily oral dose[1].
JNJ-pan-AR (30 mg/kg; p.o.; daily; 10 days) potently inhibits testosterone propionate-stimulated androgen-sensitive organ growth in mice[1].

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

Animal Model: SHO (male, castrated)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: p.o.; daily
Result: Achieved a tumor growth inhibition (TGI) of 80.2%.
Achieved a TGI of 100.8% (complete tumor growth stasis).
Reached a plasma exposure of 748 ng/mL.
Molecular Weight

515.55

Formula

C25H24F3N5O2S
CAS No.
SMILES

N#CC1=NC=C(N2C(C3(CCC3)N(C2=S)C4=CC=C(C=C4)OC5CCN(CC5)C)=O)C=C1C(F)(F)F
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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.
Purity & Documentation
References
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JNJ-pan-AR Related Classifications

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  • 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:

JNJ-pan-AR1332390-06-3Androgen ReceptorKallikreinKLKKallikrein-related peptidasewild-type androgen receptorcastration-resistant prostate cancerprostate cancer cellsVCaP prostate cancer cellsHepG2 cellsKLK2PSA proteinKLK3androgen receptorLNCaP cellsInhibitorinhibitorinhibit

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