MW:464.44
溶解性:DSMO 93 mg/mL Water <1 mg/ml Ethanol 3 mg/mL
纯度:>99%
描述:
As an androgen-receptor (AR) inhibitor, MDV3100 can inhibit AR with IC50 of 36 nM. MDV3100 impair AR nuclear translocation, DNA binding and coactivator peptide recruitment. MDV3100 can bind AR in castration-resistant LNCaP/AR human prostate cancer cells, which areengineered to express higher levels of wild-type AR to mimic the clinical scenario, with 5-8 fold greater affinity than bicalutamide. Companring to bicalutamide, MDV3100 suppressed growth and induced apoptosis whereas bicalutamide did not. MDV3100 antagonized induction of PSA and TMPRSS2 by the synthetic androgen R1881 in parental LNCaP cells. MDV3100 are orally available and induce tumor regression in mouse models of castration-resistant human prostate cancer.
参考文献:
[1] Tran C, et al.(2009) "Development of a Second-Generation Antiandrogen for Treatment of Advanced Prostate Cancer"Science.324 (5928), 787-790.
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