Abiraterone
产品说明书
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同义名 : | CB-7598 |
| CAS号 : | 154229-19-3 | |
| 货号 : | A515845 | |
| 分子式 : | C24H31NO | |
| 纯度 : | 98% | |
| 分子量 : | 349.51 | |
| MDL号 : | MFCD00924100 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 2 mg/mL(5.72 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO 无水乙醇: 5 mg/mL(14.31 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 DMF: 8 mg/mL(22.89 mM)，配合低频超声助溶 |
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| 动物实验配方： |
PO 0.5% CMC-Na 60 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The 17α-hydroxylase/C17-20 lyase (as known as CYP17A1) is a key enzyme in the androgen biosynthetic pathway. Abiraterone is a potent inhibitor of both 17α-hydroxylase and C17-20 lyase with IC50 values of 18 and 17 nM, respectively[4]. In guinea pig adrenal cells, abiraterone at the dose of 10-5 M almost completely inhibited ACTH-stimulated production of androstenedione and cortisol[5]. Moreover, abiraterone is also an inhibitor of androgen receptor (AR). It displaced ligand from wild-type AR with an EC50 value of 13.4 μM. Abiraterone (0.1 - 25 μM) also showed dose-proportional inhibitory effect on T877A-AR, G142VAR, P533S-AR, T575A-AR and H874Y-AR. In LNCaP and VCaP prostate cancer cells. Abiraterone at the concentrations of 0.1 - 5 μM decreased cell viability in a dose-dependent manner when compared to DMSO control[6]. After the treatment of LuCaP23CR and LuCaP35CR prostate cancer xenografts with abiraterone for 21 days, the serum PSA level was rapidly declined and the tumor growth was significantly inhibited as compared to vehicle-treated group. Abiraterone administration also resulted in statistically significant improvement in the progression-free survival[7]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| hamster V79MZh11B1 cells | Function assay | Inhibition of human CYP11B1 expressed in hamster V79MZh11B1 cells, IC50=1.608 μM | 18672868 | ||
| PC3 cells | Cytotoxic assay | 48 h | Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=9.32 μM | 24148837 | |
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01017939 | Prostate Neoplasms | Phase 1 | Completed | - | United States, California ... 展开 >> Tower Cancer Research Foundation Beverly Hills, California, United States, 90211 Beverly Hills, California, United States United States, Texas START - South Texas Accelerated Research Therapeutics, LLC San Antonio, Texas, United States, 78229 San Antonio, Texas, United States Canada, British Columbia BC Cancer Agency Vancouver, British Columbia, Canada, V5Z 4E6 Vancouver, British Columbia, Canada 收起 << |
| NCT03748641 | Metastatic Prostate Cancer | Phase 3 | Not yet recruiting | February 25, 2025 | - |
| NCT02090114 | Prostate Cancer | Phase 2 | Recruiting | April 2019 | United States, Maryland ... 展开 >> The Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Recruiting Baltimore, Maryland, United States, 21231 Contact: Irina Rifkind, RN, MSN 410-502-2043 irifkin1@jhmi.edu Contact: Rana Sullivan, RN, BSN 410-614-6337 tomalra@jhmi.edu Principal Investigator: Samuel Denmeade, MD 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.86mL 0.57mL 0.29mL |
14.31mL 2.86mL 1.43mL |
28.61mL 5.72mL 2.86mL |
| 参考文献 |
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