JNJ-63576253

SKU: orb1218457

Description

JNJ-63576253 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).

Key Properties

• CAS Number: 2110426-27-0
• MW: 502.51
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₁F₃N₆O₂S
• SMILES: C1CC2(C1)C(=O)N(C(=S)N2C3=CN=C(C=C3)OC4CCNCC4)C5=CC(=C(N=C5)C#N)C(F)(F)F
• Target: Androgen Receptor (AR)
• Solubility: DMSO:10 mM

Bioactivity

• 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. 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. 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. 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. Animal model: Castrated SHO mice with prostate LNCaP SRα F877L tumor. 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. 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.
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• In Vitro:
  JNJ-63576253 (0.0003-100 μM; 5 d) inhibits the growth of VCaP cells, with an IC50 of 265 nM. JNJ-63576253 is stable in human liver microsomes, with an T1/2 of >180 min.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TRC253

Quick Database Links

Gene Symbol

Androgen Receptor (AR)