Abiraterone NEW
| Price | $53 | $67 | $81 |
| Package | 10mg | 50mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-02 |
Product Details
| Product Name: Abiraterone | CAS No.: 154229-19-3 |
| Purity: 99.87% | Supply Ability: 10g |
| Release date: 2024/11/02 |
Product Introduction
Bioactivity
| 名稱 | Abiraterone |
| 描述 | Abiraterone (CB-7598) (CB-7598) is an effective steroidal cytochrome P450 17alpha-hydroxylase-17, 20-lyase (CYP17) inhibitor (IC50: 4 nM). |
| 細胞實驗 | LNCaP and VCaP cells are seeded in 96-well plates and grown in CSS-supplemented phenol red-free or FBS-supplemented media for 7 days. Cells are treated with Abiraterone at 24 hours and 96 hours after plating and cell viability is determined on day 7 by adding CellTiter Glo and measuring luminescence.(Only for Reference) |
| 激酶實驗 | C17,20-lyase activity assay: Microsomes are diluted to a final protein concentration of 50 μg/mL in the reaction mixture which contained 0.25 M sucrose, 20 mM Tris–HCl (pH 7.4), 10 mM G6P and 1.2 IU/mL G6PDH. After equilibration at 37 °C for 10 minutes, the reaction is initiated by addition of βNADP to obtain a final concentration of 0.6 mM. Prior to the distribution of 600 μL of the reaction mixture in each tube, Abiraterone is evaporated to dryness under a stream of nitrogen and then are incubated at 37 °C for 10 minutes. After incubation with Abiraterone, 500 μL of the reaction mixture is transferred to tubes containing 1 μM of the enzyme substrate, 17OHP. After a further 10 minutes incubation, tubes are placed on ice and the reaction is stopped by addition of 0.1 ml NaOH 1N. Tubes are deep-frozen and stored at ?20 °C until assayed for Δ4A levels. A Δ4A RIA is developed and automated on a microplate format using a specific antibody against Δ4A. The separation of free and bound antigen is achieved with a dextran-coated charcoal suspension. After centrifugation, aliquots of the clear supernatant are counted in duplicates in a 1450 MicrobetaPlus liquid scintillation counter. The Δ4A concentrations of unknown samples are determined from the standard curve. The detection limit is 0.5 ng/mL and the within and between assay coefficients of variation are 10.7 and 17.6%, respectively at an assay value of 13 ng/mL. The rate of enzymatic reaction is expressed as pmol of Δ4A formed per 10 minutes and per mg of protein. The value of maximum activity without inhibitor (control) is set at 100%. The IC50 values are calculated using non-linear analysis from the plot of enzyme activity (%) against log of inhibitor concentration. |
| 體外活性 | Abiraterone effectively reduces testosterone levels almost to the extent of testicular removal without significantly decreasing the size of any organ. It inhibits CYP17 in human testicular microsomes (IC50: 72 nM), leading to a reduction in testosterone levels by over 95% compared to the control group. |
| 體內活性 | Abiraterone inhibits the proliferation in vitro and the androgen receptor-mediated gene expression in androgen receptor-positive prostate cancer cells, likely through the suppression of steroidogenesis and anti-androgen receptor activity. At higher concentrations, Abiraterone inhibits the activation of mutant androgen receptors by enzalutamide. Abiraterone effectively replaces the ligand in WT-AR (EC50: 13.4 μM) and T877A mutant receptors (EC50: 7.9 μM). Additionally, Abiraterone acetate significantly suppresses testosterone secretion by 48% and increases LH levels to 192%. Abiraterone also inhibits the lysosomal activity in rat testicular microsomes (IC50: 5.8 nM). |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : 5.4 mg/mL (15.45 mM), Sonication is recommended. DMF : 8.75 mg/mL (25.04 mM), Sonication and heating are recommended. DMSO : 1 mg/mL, Sonication is recommended. |
| 關鍵字 | Inhibitor | Cytochrome P450 | CB 7598 | inhibit | CYPs | CB7598 | Abiraterone |
| 相關產品 | Naringin | Naringenin |
| 相關庫 | 經典已知活性庫 | EMA 上市藥物庫 | 藥物功能重定位化合物庫 | 已知活性化合物庫 | 抗癌藥物庫 | 抗癌活性化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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