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Proxalutamide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Proxalutamide图片
CAS NO:1398046-21-3
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
GT0918
产品介绍
Proxalutamide是具有口服活性的雄激素受体的拮抗剂。它可研究前列腺癌和COVID-19。

产品描述

Proxalutamide is a potent antagonist of the androgen receptor (AR).

体外活性

Proxalutamide inhibits the proliferation of hormone-sensitive CaP cells and more potently inhibits the proliferation of CRPC cells. Proxalutamide inhibits the growth of AR-positive breast cancer cells. Proxalutamide more effectively inhibits androgen binding with AR's ligand-binding domain than Bicalutamide (11.4x) and MDV3100 (3.5x). Proxalutamide displays stronger potency to block AR function of gene transcription than Bicalutamide (~5-10) and MDV3100 (2-5x) while maintaining full antagonism in CRPC cells, in both hormone-sensitive (LNCaP) and CRPC (C4-2) cancer cells. Proxalutamide has minimum effects on the growth of AR-negative CaP cells (PC-3 and DU145), showing it is a selective AR pathway inhibitor. Proxalutamide impairs androgen stimulates AR translocation to cell nuclei hence blocks its binding DNA and shuts down the downstream oncogenic signaling and Proxalutamide also causes AR downregulation in prostate cancer cells [1].

体内活性

The mean Proxalutamide (GT0918) half-life estimate from the pHM-SD tablets (7.9±2.2 h) was similar to that of the conventional tablets (8.4±0.5 h), remaining consistent with the following pharmacokinetic theory: the extent and rate of absorption should not affect elimination. The relative bioavailability (frel) of the pHM-SD tablets is 125.6% of that for the conventional tablets on average, revealing that the bioavailability of the former is higher. The tmax for the pHM-SD and conventional tablets are 0.9±0.4 h and 2.5±1.1 h, respectively, meaning that the pHM-SD tablets dissolve more quickly than the conventional tablets. The mean Cmax and the AUC0-36 are 5.1±2.4 μg/mL and 38.3±8.2 μgh/mL for the pHM-SD tablets versus 3.1±1.5 μg/mL and 42.1±22.3 μgh/mL for conventional tablets, respectively [2].

Cas No.

1398046-21-3

分子式

C24H19F4N5O2S

分子量

517.5

别名

GT0918

储存和溶解度

DMSO:100 mg/mL (193.24mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years