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编 号:F194492
分子式:C10H10Br2N4OS
分子量:394.09
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer.

体内研究:
在 LNCaP 异种移植模型中,VPC-14449 (100 mg/kg;每天腹腔注射两次,持续 4 周) 在总持续时间为 4 周的情况下减小肿瘤体积并消除 PSA 产生,且体重没有降低。Animal Model:Nude mice (Harlan Sprague-Dawley; 25-31 g; 6-8 weeks) were subcutaneously inoculated with LNCaP cells and castrated
Dosage:100 mg/kg
Administration:I.p. twice daily for 4 weeks
Result:Suppressed LNCaP tumor volume and blocked serum PSA production.

体外研究:
VPC-14449 (0.01-100 μM;24 小时) 抑制 LNCaP、C4-2、MR49F 和 22Rv1 细胞中的 AR 转录活性和细胞活力。 VPC-14449 (0.01-100 μM;24 h) 剂量依赖性地抑制 PC3 细胞中瞬时表达的全长人 AR (IC50=0.34 μM) 而不影响 AR 蛋白表达。
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