TRC253
- Product NameTRC253
- CAS2110426-27-0
- CBNumberCB63371325
- MFC23H21F3N6O2S
- MW502.51
- MDL NumberMFCD31922706
- MOL File2110426-27-0.mol
- MSDS FileSDS
Chemical Properties
| Boiling point | 672.3±65.0 °C(Predicted) |
| Density | 1.53±0.1 g/cm3(Predicted) |
| pka | 9.56±0.10(Predicted) |
| FDA UNII | GNG9GQ9Y27 |
TRC253 Price
| Product number | Packaging | Price | Product description | Buy |
|---|---|---|---|---|
| Matrix Scientific 233485 | 5.00mg | $1034 | 5-(8-Oxo-5-(6-(piperidin-4-yloxy)pyridin-3-yl)-6-thioxo-5,7-diazaspiro[3.4]octan-7-yl)-3-(trifluoromethyl)picolinonitrile |
Buy |
| Matrix Scientific 233485 | 10.00mg | $1540 | 5-(8-Oxo-5-(6-(piperidin-4-yloxy)pyridin-3-yl)-6-thioxo-5,7-diazaspiro[3.4]octan-7-yl)-3-(trifluoromethyl)picolinonitrile |
Buy |
| aablocks AA01W7IG | 5mg | $95 | 5-(8-Oxo-5-(6-(piperidin-4-yloxy)pyridin-3-yl)-6-thioxo-5,7-diazaspiro[3.4]octan-7-yl)-3-(trifluoromethyl)picolinonitrile ≥98% |
Buy |
| aablocks AA01W7IG | 10mg | $150 | 5-(8-Oxo-5-(6-(piperidin-4-yloxy)pyridin-3-yl)-6-thioxo-5,7-diazaspiro[3.4]octan-7-yl)-3-(trifluoromethyl)picolinonitrile ≥98% |
Buy |
| aablocks AA01W7IG | 25mg | $293 | 5-(8-Oxo-5-(6-(piperidin-4-yloxy)pyridin-3-yl)-6-thioxo-5,7-diazaspiro[3.4]octan-7-yl)-3-(trifluoromethyl)picolinonitrile ≥98% |
Buy |
TRC253 Chemical Properties,Usage,Production
Uses
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].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].
| 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 μgh/mL. |
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. DOI:10.1021/acs.jmedchem.0c01563Preparation Products And Raw materials
TRC253 Suppliers
Global(35)Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| 0510-83588313-811 18800520310 |
sales@chemshuttle.com | China | 2999 | 62 | |
| 027-87465837 19945049750 |
sales@finetechnology-ind.com | China | 9329 | 58 | |
| 021-52996696，15000506266 15000506266 |
China | 4865 | 55 | ||
| 021-61350663 13052117465 |
sales@zehanbiopharma.com | China | 989 | 55 | |
| 18916372613 | yanzihan@shyuanye.com | China | 87240 | 60 | |
| 177-54423994 17754423994 |
2853530910@QQ.com | China | 7996 | 62 | |
| 021-31433387 15618786686 |
sales@rechemscience.com | China | 2961 | 58 | |
| 15006117673 | 2973592490@qq.com | China | 271 | 58 | |
| +86-27-8746-5837 +86-18627785180 |
info@finetechnology-ind.com | China | 9533 | 58 | |
| +1-781-999-5354; +1-00000000000 |
marketing@targetmol.com | United States | 32431 | 58 |
View Latest Prices from TRC253 manufacturers
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