货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V49592-1ml	10mM in DMSO	￥2910.00 V49592-1ml ￥2910.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V49592-1ml

10mM in DMSO

￥2910.00

货期：3-5天

产品描述：

Proxalutamide (GT0918) 是第二代androgen receptor拮抗剂，在 AR 竞争性结合试验中以 32 nM 的 IC50 与 AR 的配体结合域结合

靶点：

Androgen Receptor(in the AR competive binding assay):32 nM

体外研究：

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.

体内研究：

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%

细胞实验：

Cell lines: LNCaP cells Concentrations: 0.32, 0.16, 0.8, 4, 20 mM Incubation Time: 7 days Method: LNCaP cells are seeded at a density of 2×10³ cells/ well in 96-well plates and incubated overnight for attachment. LNCaP cells are treated with Proxalutamide (0.32, 0.16, 0.8, 4 and 20 mM) for 7 d. After 20 ml of MTT solution (5 mg/ml) is added and incubated for 4 h at 37 C, the medium is removed. Then 150 ml of dimethyl sulfoxide (DMSO) is added to each well to dissolve formazan crystals by constant shaking for 10 min. The plates are read at 540 nm on a microplate reader and a doseeresponse curve is used to assess IC50.

动物实验：

Animal Models: Sprague–Dawley rats Dosages: 20 mg/kg Administration: o.g., i.v.

参考文献：

1. Tie Zhou, et, al. Preclinical profile and phase I clinical trial of a novel androgen receptor antagonist GT0918 in castration-resistant prostate cancer. Eur J Cancer. 2020 Jul;134:29-40. 2. Sang H, et al. Quantitative determination of proxalutamide in rat plasma and tissues using liquid chromatography/tandem mass spectrometry. Rapid Commun Mass Spectrom. 2021 Feb 15;35(3):e9003.

溶解性：

Soluble in DMSO、Ethanol

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.932 ml	9.662 ml	19.324 ml
5 mM	0.386 ml	1.932 ml	3.865 ml
10 mM	0.193 ml	0.966 ml	1.932 ml
50 mM	0.039 ml	0.193 ml	0.386 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

质检证书(COA)

输入产品批号：

如何获取质检证书(COA)?

请输入货号和一个与之匹配的批号。
例如:
批号：JS298415 货号：S20001-25g
在货品标签上如何找到货号和批号?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置