JNJ-63576253(TRC-253)
- CAS No.
- 2110428-64-1
- Chemical Name:
- JNJ-63576253(TRC-253)
- Synonyms
- JNJ63576253 HCl;JNJ-63576253(TRC-253);TRC-253,mutant,JNJ 63576253,resistant,wild-type,JNJ63576253,TRC 253,prostate,inhibit,Androgen Receptor,castration,cancer,Inhibitor,androgen,CRPC,LNCaP,JNJ-63576253,TRC253
- CBNumber:
- CB19383079
- Molecular Formula:
- C23H22ClF3N6O2S
- Molecular Weight:
- 538.97
- MDL Number:
- MFCD33548920
- MOL File:
- 2110428-64-1.mol
JNJ-63576253(TRC-253) Chemical Properties,Uses,Production
Biological Activity
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]. 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]. 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].
References
[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.
JNJ-63576253(TRC-253) Preparation Products And Raw materials
Raw materials
Preparation Products
JNJ-63576253(TRC-253) Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
| Wuhan Acumen Bio-Technology Co.,ltd | 027-027-16602739303 16602739303 | 673003916@qq.com | China | 2927 | 58 |
| Shanghai Lollane Biological Technology Co.,Ltd. | 021-52996696，15000506266 15000506266 | China | 4153 | 55 | |
| Shanghai Rechem science Co., Ltd. | 21-31433387 15618786686 | sales@rechemscience.com | China | 2993 | 58 |
| Shanghai Chaolan Chemical Technology Center | QQ:65489617 15618227136 | info@SuperLan-chem.com | China | 9767 | 58 |
| Shanghai SuperLan Chemcial Technique Centre | 021-2022843681 15618226720 | chaolaichem@foxmail.com | China | 9038 | 58 |