| Identification | Back Directory | [Name]
JNJ-63576253(TRC-253) | [CAS]
2110428-64-1 | [Synonyms]
JNJ63576253 HCl
JNJ-63576253(TRC-253) | [Molecular Formula]
C23H22ClF3N6O2S | [MDL Number]
MFCD33548920 | [MOL File]
2110428-64-1.mol | [Molecular Weight]
538.97 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 250 mg/mL (463.85 mM; Need ultrasonic) | [form ]
Solid | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [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]. | [storage]
Store at -20°C | [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. |
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| Company Name: |
DC Chemicals
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| Tel: |
021-58447131 13564518121 |
| Website: |
https://www.chemicalbook.com/ShowSupplierProductsList927327/0.htm |
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