JNJ-63576253 free base
Based on 1 publication(s) in Google Scholar
JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC).
For research use only. We do not sell to patients.
- CAS No.: 2110426-27-0
- Formula: C23H21F3N6O2S
- Molecular Weight:502.51
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) JNJ-63576253 free base
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Biological Activity
IC50: 37 nM (F877L mutant AR in LNCaP cells); 54 nM (wild-type AR in LNCaP cells)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| VCaP | IC50 |
265 nM
Compound: 5; JNJ-63576253
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Antiproliferative activity against human VCaP cells expressing wild-type androgen receptor assessed as reduction in cell viability incubated for 5 days in presence of R1881 by CellTiter-glo assay
Antiproliferative activity against human VCaP cells expressing wild-type androgen receptor assessed as reduction in cell viability incubated for 5 days in presence of R1881 by CellTiter-glo assay
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[PMID: 33470111] |
| VCaP | IC50 |
290 nM
Compound: 110; JNJ-63576253
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Antiproliferative activity against human VCaP cells
Antiproliferative activity against human VCaP cells
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[PMID: 35786895] |
JNJ-63576253 (30 mg/kg; p.o. once daily for 10 days) inhibits the five androgen sensitive organs (ASOs) under stimulation by testosterone propionate (TP) in mice[1].
JNJ-63576253 (10 mg/kg; p.o.) exhibits moderate oral bioavailability (45%), Cmax (0.66 μM) and AUClast (4.9 μg h/mL) in mice[1].
JNJ-63576253 (2 mg/kg; i.v.) exhibits reasonable half-life (5.99 h), CL (15.0 mL/min/kg) and Vdss (6.11 L/kg) in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Castrated SHO mice with prostate LNCaP SRα F877L tumor[1]
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Dosage:30 mg/kg
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Administration:P.o. once daily for 72 days
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Result:Inhibited the tumor growth by 87%.
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Animal Model:CD-1 male mice[1]
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Dosage:2 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
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Administration:Intravenous administration and oral administration
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Result:I.v.: T1/2=5.99 h; CL=15.0 mL/min/kg; Vdss=6.11 L/kg.
P.o.: F=45%; Cmax=0.66 μM; AUClast=4.9 μg•h/mL.
Chemical Information
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CAS No. 2110426-27-0
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Molecular Weight 502.51
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Formula C23H21F3N6O2S
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SMILES
O=C(N(C(N1C2=CC=C(N=C2)OC3CCNCC3)=S)C(C=C4C(F)(F)F)=CN=C4C#N)C51CCC5
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Synonyms
TRC-253 free base
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Eur J Med Chem
Elevated labile iron in castration-resistant prostate cancer is targetable with ferrous iron-activatable antiandrogen therapy. [Abstract]2023 Mar 5:249:115110. PMID: 36708680
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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