1. Others
  2. Androgen Receptor
  3. JNJ-63576253

JNJ-63576253 (Synonyms: TRC-253)

Cat. No.: HY-115282
Handling Instructions

JNJ-63576253 (TRC-253) 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 can be used for the research of castration-resistant prostate cancer (CRPC).

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

JNJ-63576253 Chemical Structure

JNJ-63576253 Chemical Structure

CAS No. : 2110426-27-0

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other In-stock Forms of JNJ-63576253:

Other Forms of JNJ-63576253:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

JNJ-63576253 (TRC-253) 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 can be used for the research of castration-resistant prostate cancer (CRPC)[1].

IC50 & Target

IC50: 37 nM (F877L mutant AR in LNCaP cells); 54 nM (wild-type AR in LNCaP cells)[1]

In Vitro

JNJ-63576253 (0.0003-100 μM; 5 d) inhibits the growth of VCaP cells, with an IC50 of 265 nM[1].
JNJ-63576253 is stable in human liver microsomes, with an T1/2 of >180 min[1].

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

In Vivo

JNJ-63576253 (30 mg/kg; p.o. once daily for 72 days) significantly inhibits the growth of prostate LNCaP SRα F877L tumor in mice[1].
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].

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

Animal Model: Castrated SHO mice with prostate LNCaP SRα F877L tumor[1]
Dosage: 30 mg/kg
Administration: P.o. once daily for 72 days
Result: Inhibited the tumor growth by 87%.
Animal Model: CD-1 male mice[1]
Dosage: 2 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
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.
Molecular Weight

502.51

Formula

C₂₃H₂₁F₃N₆O₂S

CAS No.

2110426-27-0

SMILES

O=C(N(C(N1C2=CC=C(N=C2)OC3CCNCC3)=S)C(C=C4C(F)(F)F)=CN=C4C#N)C51CCC5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

JNJ-63576253TRC-253JNJ63576253JNJ 63576253TRC253TRC 253Androgen ReceptorandrogenARmutantwild-typeLNCaPcastrationresistantprostatecancerCRPCInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
JNJ-63576253
Cat. No.:
HY-115282
Quantity:
MCE Japan Authorized Agent: