N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide
- CAS No.
- 915087-27-3
- Chemical Name:
- N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide
- Synonyms
- RD 162;Depyridinyl Phenyl Apalutamide;N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide;Benzamide, 4-[7-[4-cyano-3-(trifluoromethyl)phenyl]-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methyl-;inhibit,prostate,RD-162,Androgen Receptor,VCaP,Inhibitor,castration,NSAA,LNCaP,diarylthiohydantoin,RD162,orally,RD 162
- CBNumber:
- CB02651309
- Molecular Formula:
- C22H16F4N4O2S
- Molecular Weight:
- 476.45
- MDL Number:
- MOL File:
- 915087-27-3.mol
- MSDS File:
- SDS
N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide Properties
Melting point | >170°C (dec.) |
---|---|
Density | 1.55 |
storage temp. | -20°C Freezer, Under inert atmosphere |
solubility | Chloroform (Slightly), Methanol (Slightly) |
form | Solid |
color | White to Pale Yellow |
FDA UNII | 5ZE6THH5VF |
N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide price More Price(12)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 13039 | RD162 ≥98% | 915087-27-3 | 1mg | $34 | 2024-03-01 | Buy |
Cayman Chemical | 13039 | RD162 ≥98% | 915087-27-3 | 5mg | $157 | 2024-03-01 | Buy |
Cayman Chemical | 13039 | RD162 ≥98% | 915087-27-3 | 10mg | $297 | 2024-03-01 | Buy |
Cayman Chemical | 13039 | RD162 ≥98% | 915087-27-3 | 25mg | $656 | 2024-03-01 | Buy |
American Custom Chemicals Corporation | API0007616 | RD 162 95.00% | 915087-27-3 | 5MG | $303.6 | 2021-12-16 | Buy |
N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide Chemical Properties,Uses,Production
Uses
Depyridinyl Phenyl Apalutamide is a derivative of Apalutamide(A726120) which is a second-generation antiandrogen used in the treatment of prostate cancer.
Biological Activity
rd162 is an androgen receptor (ar) antagonist.metastatic prostate cancer is treated with drugs antagonizinf androgen action, but most patients progress to a more aggressive form of the disease named castration-resistant prostate cancer, driven by elevated expression of the androgen receptor (ar).
in vitro
rd162 was optimized from a screen for nonsteroidal antiandrogens retaining activity in the setting of increased androgen receptor expression. rd162 could bind to the androgen receptor with greater relative affinity than the clinically used bicalutamide, reduce the efficiency of the nuclear translocation, and impair both dna binding to androgen response elements and recruitment of coactivators [1].
in vivo
previous evidence suggested that the activity of rd162 in these mice was mediated through ar inhibition. the antitumor activity in the lncap/ar model was dose-dependent, with some slowing of tumor growth at 0.1 mg/kg rd162 and a few tumor regressions at 1 mg/kg, correlating closely with the effect of these same doses on ar transcriptional activity in the luciferase imaging experiment. in addition, neither bicalutamide nor rd162 impaired the growth of ar-negative du145 prostate cancer xenografts [1].
IC 50
30.9 nm
References
[1] c. tran, s. ouk, n. j. clegg, et al. development of a second-generation antiandrogen for treatment of advanced prostate cancer. science 324(5928), 787-790(2009).
N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide Preparation Products And Raw materials
Raw materials
Preparation Products
N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Aceschem Inc. | +1-817863-6948 +1-(817)863-6948 | sales@aceschem.com | United States | 19639 | 58 |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131980 | 58 |
Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9707 | 58 |
ShangHai Biochempartner Co.,Ltd | 17754423994 17754423994 | 2853530910@QQ.com | China | 8014 | 62 |
Shanghai Chaolan Chemical Technology Center | QQ:65489617 15618227136 | info@SuperLan-chem.com | China | 9943 | 58 |
Amatek Scientific Co. Ltd. | 0512-56316828 | info@amateksci.com | China | 28817 | 58 |
BOC Sciences | -- | info@bocsci.com | USA | 0 | 65 |
Shanghai Dongyang Biotechnology Co., Ltd. | 0512-0512-13601744364 13601744364 | chemsharker@126.com | China | 902 | 58 |
ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11289 | 58 |