Abiraterone Acetate
产品说明书
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同义名 : | 醋酸阿比特龙酯 ;CB7630; CB7630 Acetate |
| CAS号 : | 154229-18-2 | |
| 货号 : | A726525 | |
| 分子式 : | C26H33NO2 | |
| 纯度 : | 98% | |
| 分子量 : | 391.546 | |
| MDL号 : | MFCD00934213 | |
| 存储条件： |
Pure form Sealed in dry, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 9 mg/mL(22.99 mM)，配合低频超声助溶，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 |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+30% PEG300+water 0.4 mg/mL clear PO 0.5% CMC-Na 38 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Abiraterone acetate is an ester prodrug of Abiraterone, a potent anticancer agent that exhibits IC50 values of 15 nM for 17,20-lyase and 2.5 nM for 17α-hydroxylase, both activities of the bifunctional enzyme CYP17. In its active form, Abiraterone specifically inhibits human 17,20-lyase and 17α-hydroxylase with IC50 values of 27 nM and 30 nM, respectively[1]. Abiraterone significantly inhibits the proliferation of androgen receptor-positive prostate cancer cell lines LNCaP and VCaP at doses ≥5 μM[2]. Abiraterone also inhibits the activity of recombinant human 3β-hydroxysteroid dehydrogenase types 1 and 2 (3βHSD1 and 3βHSD2), with competitive Ki values of 2.1 μM and 8.8 μM respectively. At a concentration of 10 μM, Abiraterone completely blocks the synthesis of 5α-dione and dihydrotestosterone (DHT) in these cell lines. Furthermore, treatment with Abiraterone significantly inhibits the progression of castration-resistant prostate cancer (CRPC), effectively capping tumor growth over a 4-week treatment period with highly significant results (P<0.00001)[3]. | ||
| 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 V79MZh cells | Function assay | Inhibition of human CYP11B1 expressed in hamster V79MZh cells, IC50=1.61 μM | 20550118 | ||
| hamster V79MZh11B1 cells | Function assay | Inhibition of human CYP11B1 expressed in hamster V79MZh11B1 cells, IC50=1.608 μM | 18672868 | ||
| human 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 |
| NCT01957436 | Metastatic Prostate Cancer | Phase 3 | Recruiting | December 2030 | - |
| NCT02160353 | High Risk Localised Prostate C... 展开 >>arcinoma 收起 << | Phase 2 | Recruiting | October 2020 | Ireland ... 展开 >> Cork University Hospital Recruiting Cork, Ireland Contact: Contact Person 021-4920014 Principal Investigator: Paul Kelly, Dr St Luke's Hospital Recruiting Dublin, Ireland, 6 Contact: Contact Person 01-4065000 Principal Investigator: Pierre Thirion, Dr University Hospital Galway Recruiting Galway, Ireland Contact: Contact Person 091-893487 Principal Investigator: Cormac Small, Dr 收起 << |
| NCT02656615 | Prostate Cancer | Phase 2 | Terminated(Lack of Patient acc... 展开 >>rual) 收起 << | - | Switzerland ... 展开 >> Cantonal Hospital Chur Chur, Graubuenden, Switzerland, 7000 University Hospital Basel Basel, Switzerland, 4000 Cantonal Hospital St.Gallen St.Gallen, Switzerland, 9007 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.55mL 0.51mL 0.26mL |
12.77mL 2.55mL 1.28mL |
25.54mL 5.11mL 2.55mL |
| 参考文献 |
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