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TOK-001 (VN/124-1; Galeterone) is a multifunctional antiandrogen and CYP17 inhibitor(IC50=47 nM) in castration resistant prostate cancer (CRPC).TOK-001 and abiraterone reduced AR protein and mRNA expression, and antagonized AR-dependent promoter activation induced by androgen. TOK-001, but not abiraterone, is an effective apparent competitor of the radioligand [(3)H]R1881 for binding to the wild type and various mutant AR (W741C, W741L) proteins. TOK-001 is a consistently superior inhibitor than abiraterone of R1881-induced transcriptional activity of both wild type and mutant AR. For the detailed information of TOK-001(Galeterone), the solubility of TOK-001(Galeterone) in water, the solubility of TOK-001(Galeterone) in DMSO, the solubility of TOK-001(Galeterone) in PBS buffer, the animal experiment (test) of TOK-001(Galeterone), the cell expriment (test) of TOK-001(Galeterone), the in vivo, in vitro and clinical trial test of TOK-001(Galeterone), the EC50, IC50,and affinity,of TOK-001(Galeterone), Please contact DC Chemicals. |