Abiraterone
(Synonyms: 阿比特龙,CB 7598,16-dien-3-ol,CB7598) 目录号 : GC17645
Abiraterone是一种FDA批准的CYP17A1抑制剂，已获批准用于去势抵抗性前列腺癌（CRPC）的治疗。
Cas No.:154229-19-3
Sample solution is provided at 25 µL, 10mM.
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Abiraterone, a CYP17A1 inhibitor approved by the FDA, has been approved for the treatment of castration-resistant prostate cancer (CRPC)[1].
In vitro, Abiraterone (20 or 40μM; 72h) treatment significantly reduced mitochondrial respiration in T98G and U87MG-R cells[2]. The antiandrogen Abiraterone (0, 1, 5, 10 and 20μM; 72h) in combination with inhibitors of Polo-like kinase 1 synergistically kills CRPC cells[3].
In vivo, In an orthotopic brain tumor mouse model, co-administration of Abiraterone (10mg/kg; once every three days; i.p.) and Progesterone significantly curtailed the progression of implanted U87MG-R-luc GBM tumors[2]. The use of the small-molecule inhibitor Abiraterone (10mg/kg; 20 days; i.p.) to reduce testosterone synthesis significantly enhanced the antitumor activity of T cells in male mice and improved the efficacy of anti-PD-1 immunotherapy[4].
References:
[1] Lu D, Song Y, Yu Y, et al. KAT2A-mediated AR translocation into nucleus promotes abiraterone-resistance in castration-resistant prostate cancer. Cell Death Dis. 2021 Aug 12;12(8):787.
[2] Chen HC, Lin HY, Chiang YH, et al. Progesterone boosts abiraterone-driven target and NK cell therapies against glioblastoma. J Exp Clin Cancer Res. 2024 Aug 6;43(1):218.
[3] Patterson JC, Varkaris A, Croucher PJP, et al. Plk1 Inhibitors and Abiraterone Synergistically Disrupt Mitosis and Kill Cancer Cells of Disparate Origin Independently of Androgen Receptor Signaling. Cancer Res. 2023 Jan 18;83(2):219-238.
[4] Zhang X, Cheng L, Gao C, et al. Androgen Signaling Contributes to Sex Differences in Cancer by Inhibiting NF-κB Activation in T Cells and Suppressing Antitumor Immunity. Cancer Res. 2023 Mar 15;83(6):906-921.
Abiraterone是一种FDA批准的CYP17A1抑制剂，已获批准用于去势抵抗性前列腺癌（CRPC）的治疗[1]。
在体外实验中，Abiraterone（20或40μM; 72小时）处理显著降低了T98G和U87MG-R细胞的线粒体呼吸[2]。抗雄激素Abiraterone（0, 1, 5, 10和20μM; 72小时）与Polo样激酶1抑制剂联合使用可协同杀死去势抵抗性前列腺癌细胞[3]。
在体内实验中，在原位脑肿瘤小鼠模型中，Abiraterone（10mg/kg; 每3天给药一次; 腹腔注射）与孕酮联合使用显著抑制了植入的U87MG-R-luc胶质母细胞瘤肿瘤的进展[2]。使用小分子抑制剂Abiraterone（10mg/kg; 20天; 腹腔注射）减少睾酮合成显著增强了雄性小鼠中T细胞的抗肿瘤活性，并提高了抗PD-1免疫疗法的疗效[4]。
| Cell experiment [1]: | |
Cell lines | C4-2 cells |
Preparation Method | C4-2 cells were plated in 96- or 384-well plates at a density of 4000 or 1000 cells per well in 95µl or 22.5µl of medium, respectively. On the following day, drugs were added to the wells after being diluted in 5µl or 2.5µl of medium (for 96- or 384-well plates, respectively). The concentrations of Abiraterone were 0, 1, 5, 10 and 20μM, and those of BI2536 (Plk1 inhibitor) were 0, 1, 10 and 50μM. A constant amount of DMSO vehicle was maintained in all wells. After 72h of incubation, cell viability relative to the control was measured using CellTiter-Glo™ according to the manufacturer’s recommendations. Luminescence in individual wells in plates with opaque walls was measured using the Infinite™ M200 Pro plate reader. Relative viability was calculated by dividing the luminescent signal from each well by that measured in the vehicle-control well on an individual replicate basis. For experiments examining cell number and relative confluence, drug-treated cells were washed with PBS and fixed with 4% formaldehyde for 1h, stained with 1µM SYTO™ 60, and imaged on the Odyssey™ CLx scanner. |
Reaction Conditions | 0, 1, 5, 10 and 20μM; 72h |
Applications | The antiandrogen Abiraterone (0, 1, 5, 10 and 20μM; 72h) in combination with inhibitors of Polo-like kinase 1 synergistically kills CRPC cells. |
| Animal experiment [2]: | |
Animal models | NOD.CB17-Prkdcscid/NCrCrl mice (8-week-old) and C57BL/6 mice (8-week-old) |
Preparation Method | On Day 0, 5 × 10⁵ GBM cells were collected in 5µl of medium and implanted into the mouse brain using a stereotactic instrument and micro-injector. Starting on Day 6, the mice were divided into three groups: untreated control group, Abiraterone-only group (10mg/kg), and Abiraterone (10mg/kg) + Progesterone combination group. The drugs were administered via intraperitoneal injection (once every three days) until the death of the mice. For IVIS imaging, mice were injected intraperitoneally with 200µl of luciferin (15mg/ml) and then imaged using the IVIS Lumina III XRMS. |
Dosage form | 10mg/kg; once every three days; i.p. |
Applications | In an orthotopic brain tumor mouse model, co-administration of Abiraterone (10mg/kg; once every three days; i.p.) and Progesterone significantly curtailed the progression of implanted U87MG-R-luc GBM tumors. |
References: | |
| Cas No. | 154229-19-3 | SDF | |
| 别名 | 阿比特龙,CB 7598,16-dien-3-ol,CB7598 | ||
| 化学名 | (3S,8R,9S,10R,13S,14S)-10,13-dimethyl-17-pyridin-3-yl-2,3,4,7,8,9,11,12,14,15-decahydro-1H-cyclopenta[a]phenanthren-3-ol | ||
| Canonical SMILES | CC12CCC(CC1=CCC3C2CCC4(C3CC=C4C5=CN=CC=C5)C)O | ||
| 分子式 | C24H31NO | 分子量 | 349.52 |
| 溶解度 | 15 mg/ml in DMF; 1 mg/ml in DMSO; 15 mg/ml in Ethanol | 储存条件 | Store at -20°C;Argon filled and protected from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8611 mL | 14.3053 mL | 28.6107 mL |
| 5 mM | 0.5722 mL | 2.8611 mL | 5.7221 mL |
| 10 mM | 0.2861 mL | 1.4305 mL | 2.8611 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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