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产品详情
产品名称 英文名称:AZD3514 同义词 AZD3514、1240299-33-5、AZD-3514、1-(4-(2-(4-(1-(3-(Trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)piperazin-1-yl)ethanone、CS-1443、127DSS8X7J、CHEMBL2346976、AZD 3514 [WHO-DD]、1-[4-[2-[4-[1-[3-(trifluoromethyl)-7, 产品性质 CAS编号:1240299-33-5 分子式:C25H32F3N7O2 分子量:519.56 PubChem编号:46893585 英文别名:AZD3514|1240299-33-5|AZD-3514|1-(4-(2-(4-(1-(3-(Trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)piperazin-1-yl)ethanone|CS-1443|127DSS8X7J|CHEMBL2346976|AZD 3514 [WHO-DD]|1-[4-[2-[4-[1-[3-(trifluoromethyl)-7, 规格或纯度:≥98% 英文名称:AZD3514 生化机理:DescriptionIC50 Value N/AAZD3514 is a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer [1]. AZD3514 binds to the AR ligand binding domain and has selectivity for binding to AR over other nuclear hormone receptors.in vitro AZD3514 inhibits cell growth in prostate cancer cells expressing wild-type (VCaP) and mutated (T877A) AR (LNCaP), but is inactive in AR-negative prostate cancer cells, indicating a dependency on AR for efficacy [2].in vivo We assessed activity initially in the Hershberger castrated rat assay in which oral dosing of AZD3514 (100mg/kg once-daily for 7 days) significantly inhibited testosterone-induced growth of sexual accessory organs [2].Clinical trial Open-label Prostate Cancer Study. Phase 1 储存温度:-20°C储存 运输条件:超低温冰袋运输 产品介绍:AZD3514是口服的雄激素受体负调节剂,Ki为2.2 μM,可降低AR蛋白的表达。AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression. ALogP:1.7 IUPAC Name:1-[4-[2-[4-[1-[3-(trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl]piperidin-4-yl]phenoxy]ethyl]piperazin-1-yl]ethanone INCHI:InChI=1S/C25H32F3N7O2/c1-18(36)33-14-12-32(13-15-33)16-17-37-21-4-2-19(3-5-21)20-8-10-34(11-9-20)23-7-6-22-29-30-24(25(26,27)28)35(22)31-23/h2-5,20H,6-17H2,1H3 InChi Key:JMEYDSHPKCSIJC-UHFFFAOYSA-N Canonical SMILES:CC(=O)N1CCN(CC1)CCOC2=CC=C(C=C2)C3CCN(CC3)C4=NN5C(=NN=C5C(F)(F)F)CC4 Isomeric SMILES:CC(=O)N1CCN(CC1)CCOC2=CC=C(C=C2)C3CCN(CC3)C4=NN5C(=NN=C5C(F)(F)F)CC4 PubChem CID:46893585 溶解性:25°C DMSO 象形图: 信号词:Danger 危险声明:H301 Toxic if swallowed 预防措施声明:P321,P405,P501,P264,P270,P330,P301+P316 产品包装
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