JNJ63576253

SKU: orb1218456

Description

JNJ-63576253 is a Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC).

Key Properties

• CAS Number: 2110428-64-1
• MW: 538.97
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₂ClF₃N₆O₂S
• SMILES: N#CC1=NC=C(N(C2=O)C(N(C3=CC=C(OC4CCNCC4)N=C3)C52CCC5)=S)C=C1C(F)(F)F.[H]Cl
• Target: Androgen Receptor (AR)
• Solubility: DMSO: 200mg/mL (371.08 mM);H2O: insoluble

Bioactivity

• In Vivo:
  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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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

TRC-253

Quick Database Links

Gene Symbol

Androgen Receptor (AR)