Proxalutamide (GT0918)
(Synonyms: GT0918; Pruxelutamide) 目录号 : GC33224
Proxalutamide (GT0918) is a second-generation androgen receptor antagonist that binds to the ligand-binding domain of AR with an IC50 of 32 nM in the AR competive binding assays.
Cas No.:1398046-21-3
Sample solution is provided at 25 µL, 10mM.
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Proxalutamide (GT0918) is a second-generation androgen receptor antagonist that binds to the ligand-binding domain of AR with an IC50 of 32 nM in the AR competive binding assays.
Proxalutamide, a novel 2nd generation AR antagonist, binds to the ligand- binding domain of AR, with an IC50 of 32 nM in the AR competitive binding assays. Proxalutamide can block AR transcriptional activity, reduce AR protein levels, and obviously inhibit PCa growth in vitro. [1]
The elimination half-life of proxalutamide in rats is approximately 2 h regardless of whether it is administered by the intragastric or the intravenous route. The maximum plasma concentration of proxalutamide can reach 2 μg/mL or higher, and the oral absolute bioavailability is approximately 80%. [2]
[1] Tie Zhou, et, al. Eur J Cancer. 2020 Jul;134:29-40. [2] Sang H, et al. Rapid Commun Mass Spectrom. 2021 Feb 15;35(3):e9003.
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Animal experiment: |
Beagle Dogs[2]A single dose (25 mg Proxalutamide), randomized study with a two period crossover design is carried out to assess the pharmacoki-netics. Six healthy beagle dogs (9.3±0.7 kg) are randomly divided into two groups and fasted with free access to water overnight. Each group is orally administered with pHM-SDs tablet (Test) or a conventional tablet followed by 50 mL of water, respectively. The dogs obtain free access to water and food 6 h after drug administration. After a 1-week washout period, the groups are inverted and the administrations are repeated. A series of blood samples (1 mL) is collected in heparinized tubes using an indwelling cannula at pre-dose (-0.5 h) and post-dose (0.5, 1, 1.5, 2, 2.5 4, 6, 12, 24, 30, 36 and 48 h); these samples are gently mixed and centrifuged at 4000 rpm for 10 min within 1 h of collection[2]. |
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References: [1]. Youzhi Tong, et al. Abstract 614: Proxalutamide (GT0918), a potent androgen receptor pathway inhibitor. Cancer Research. AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA. |
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| Cas No. | 1398046-21-3 | SDF | |
| 别名 | GT0918; Pruxelutamide | ||
| Canonical SMILES | N#CC1=CC=C(N(C(N(C2=CC=C(CCCC3=NC=CO3)N=C2)C4(C)C)=S)C4=O)C(F)=C1C(F)(F)F | ||
| 分子式 | C24H19F4N5O2S | 分子量 | 517.5 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| 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 | 1.9324 mL | 9.6618 mL | 19.3237 mL |
| 5 mM | 0.3865 mL | 1.9324 mL | 3.8647 mL |
| 10 mM | 0.1932 mL | 0.9662 mL | 1.9324 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet