JNJ-63576253 (TRC-253) 是一种有效和具有口服活性的雄激素受体 (androgen receptor) 的完全拮抗剂，在 LNCaP 细胞中对 F877L 突变型 AR 和野生型 AR 的 IC₅₀ 值分别为 37 和 54 nM。JNJ-63576253 可用于去势抵抗性前列腺癌 (CRPC) 的研究。

JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC 50 s 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).

Solid

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

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 T 1/2 of >180 min. has not independently confirmed the accuracy of these methods. They are for reference only.

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%), C max (0.66 μM) and AUC last (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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Zhang Z, et, al. Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC). J Med Chem. 2021 Jan 28;64(2):909-924.

In Vitro: DMSO : 250 mg/mL (463.85 mM; Need ultrasonic)配制储备液