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| | JNJ-63576253(TRC-253) Basic information |
| Product Name: | JNJ-63576253(TRC-253) | | Synonyms: | JNJ-63576253(TRC-253);JNJ63576253 HCl;TRC-253,mutant,JNJ 63576253,resistant,wild-type,JNJ63576253,TRC 253,prostate,inhibit,Androgen Receptor,castration,cancer,Inhibitor,androgen,CRPC,LNCaP,JNJ-63576253,TRC253 | | CAS: | 2110428-64-1 | | MF: | C23H22ClF3N6O2S | | MW: | 538.97 | | EINECS: | | | Product Categories: | | | Mol File: | 2110428-64-1.mol |  |
| | JNJ-63576253(TRC-253) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO : 250 mg/mL (463.85 mM; Need ultrasonic) |
| | JNJ-63576253(TRC-253) Usage And Synthesis |
| 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 |
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