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My CartCAS：956104-40-8
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 956104-40-8 |
| Name | Apalutamide |
| Molecular Formula | C21H15F4N5O2S |
| Molecular Weight | 477.44 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 807-449-9 |
| MDL | MFCD22380626 |
| SMILES | O=C(NC)C1=CC=C(N(C(N(C2=CC(C(F)(F)F)=C(C#N)N=C2)C3=O)=S)C43CCC4)C=C1F |
| Target Point | Androgen Receptor |
| Passage | Endocrinology & Hormones |
| Background | Apalutamide is a selective, competitive androgen receptor inhibitor. |
| Biological Activity | Apalutamide (ARN-509) 是有效, 竞争性的 雄激素受体 (AR) 拮抗剂, IC50 为 16 nM[1]。 |
| IC50 | IC50: 16nM (Androgen receptor) [1] |
| In Vitro | 在放射性配体结合测定中，阿帕他胺(ARN-509)对GABAA受体也表现出低微摩尔亲和力(IC503μM)，因此可能在治疗剂量水平下拮抗GABAA [1]。 Apalutamide是一种有效的雄激素受体(AR)拮抗剂，其靶向AR配体结合结构域并阻止AR核转位，DNA结合和AR基因靶标的转录[2]。 |
| In Vivo | 阿帕他胺(ARN-509)在小鼠和狗中表现出低的全身清除率，高口服生物利用度和长的血浆半衰期，支持每日口服一次。与其长终末半衰期一致，重复剂量研究中阿帕他胺稳态血浆水平增加，导致高C24hr水平和低峰谷比(比率：2.5)。携带LNCaP / AR异种移植肿瘤的阉割雄性小鼠用剂量为1，10或30mg / kg /天的阿帕他胺处理。 20只阿帕他汀(30mg / kg /天)处理动物中的13只在第28天肿瘤体积减少> 50％，而19只MDV3100(30mg / kg /天)处理的小鼠中有3只[1]。 |
| Cell Experiment | 将胰蛋白酶化的VCaP细胞在无酚红RPMI 1640(含5％CSS)中调节至100，000细胞/ mL的浓度，并以16μL等分试样分配到CellBIND 384孔板中。将细胞温育48小时，然后将配体以16μL体积加入RPMI培养基中。对于拮抗剂模式测定，将配体稀释在也含有30pM R1881的培养基中。孵育7天后，加入16μLCellTiter-Glo发光细胞存活率测定并测量相对发光单位(RLU)[1]。 |
| Animal Experiment | 小鼠[1]在SHO SCID雄性小鼠中进行体内异种移植实验以确定抗肿瘤反应。在异氟烷麻醉下对小鼠进行睾丸切除术，并在肿瘤细胞注射前给予2-3天恢复。将LNCaP / AR(cs)细胞悬浮于50％RPMI，50％基质胶中，并以100μL的体积注射5×10 6个细胞/异种移植物。每周观察动物直至肿瘤生长明显。从注射后24天开始，每周测量肿瘤，并且在注射后40-60天后，将动物随机分成等长平均(150-250mm 3)和范围肿瘤负荷的群组。通过口服强饲法每天施用所有化合物(例如，阿帕鲁胺，每天30mg / kg)。使用Graphpad Prism进行统计分析。 |
| Data Literature Source | [1]. Clegg NJ， et al. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012 Mar 15; 72 (6) :1494-503. [2]. Smith MR， et al. Phase 2 Study of the Safety and Antitumor Activity of Apalutamide (ARN-509) ， a Potent Androgen Receptor Antagonist， in the High-risk Nonmetastatic Castration-resistant Prostate Cancer Cohort. Eur Urol. 2016 May 6. pii: S0302-2838 (16) 30133 |
| Unit | Bottle |
| Specification | 5mg 10mg |
是一种选择性的，竞争性androgen receptor抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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