JNJ-63576253 free base(Synonyms: TRC-253 free base)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

JNJ-63576253 free base (Synonyms: TRC-253 free base)

JNJ-63576253 (TRC-253) free base 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 free base 可用于去势抵抗性前列腺癌 (CRPC) 的研究。

JNJ-63576253 free base(Synonyms: TRC-253 free base)

JNJ-63576253 free base Chemical Structure

CAS No. : 2110426-27-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

JNJ-63576253 free base 的其他形式现货产品:

JNJ-63576253

生物活性

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)[1].

IC50 & Target

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

Shanghai Jinpan Biotech Co Ltd 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.

Clinical Trial

分子量

502.51

Formula

C23H21F3N6O2S
CAS 号

2110426-27-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务