N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide

Product Name: 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;RD162, 10 mM in DMSO;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
Formula Weight: 476.45
MOL File: 915087-27-3.mol

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N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide Property

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

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 13039
Product name: RD162
Purity: ≥98%
Packaging: 1mg
Price: $34
Updated: 2024/03/01

Cayman Chemical

Product number: 13039
Product name: RD162
Purity: ≥98%
Packaging: 5mg
Price: $157
Updated: 2024/03/01

Cayman Chemical

Product number: 13039
Product name: RD162
Purity: ≥98%
Packaging: 10mg
Price: $297
Updated: 2024/03/01

Cayman Chemical

Product number: 13039
Product name: RD162
Purity: ≥98%
Packaging: 25mg
Price: $656
Updated: 2024/03/01

ApexBio Technology

Product number: C3186
Product name: RD162
Packaging: 5mg
Price: $130
Updated: 2021/12/16

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N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide Chemical Properties,Usage,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

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N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide Suppliers

China 39 The Netherlands 1 United States 5 USA 1 Global 46

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915087-27-3, N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamideRelated Search:

N-Methyl-4-[7-(4-cyano-3-trifluoromethylphenyl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl]-2-fluorobenzamide

RD 162

Benzamide, 4-[7-[4-cyano-3-(trifluoromethyl)phenyl]-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methyl-

Depyridinyl Phenyl Apalutamide

inhibit,prostate,RD-162,Androgen Receptor,VCaP,Inhibitor,castration,NSAA,LNCaP,diarylthiohydantoin,RD162,orally,RD 162

RD162, 10 mM in DMSO

915087-27-3