915087-27-3 Usage
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).
Check Digit Verification of cas no
The CAS Registry Mumber 915087-27-3 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,1,5,0,8 and 7 respectively; the second part has 2 digits, 2 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 915087-27:
(8*9)+(7*1)+(6*5)+(5*0)+(4*8)+(3*7)+(2*2)+(1*7)=173
173 % 10 = 3
So 915087-27-3 is a valid CAS Registry Number.
915087-27-3Relevant articles and documents
IMIDAZOLIDINEDIONE COMPOUNDS AND THEIR USES
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, (2014/10/29)
Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. Said imidazolidinedione compounds posses androgen receptor antagonist activity and can be used for preventing and treating diseases and disorders related to androgen receptor, such as prostate cancer, alopecia, hair regeneration, acne and adolescent acne.
