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Proxalutamide (Synonyms: GT0918)

Cat. No.: HY-103184
Handling Instructions

GT0918 is a potent androgen receptor (AR) antagonist.

For research use only. We do not sell to patients.

Proxalutamide Chemical Structure

Proxalutamide Chemical Structure

CAS No. : 1398046-21-3

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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

GT0918 is a potent androgen receptor (AR) antagonist.

IC50 & Target

Androgen Receptor[1].

In Vitro

In biochemical assay, GT0918 more potently inhibits androgen binding with AR's ligand binding domain than Bicalutamide (11.4x) and MDV3100 (3.5x). In both hormone-sensitive (LNCaP) and CRPC (C4-2) cancer cells, GT0918 demonstrates stronger potency to block AR function of gene transcription than Bicalutamide (∼5-10) and MDV3100 (2-5x) while maintaining full antagonism in CRPC cells. GT0918 impairs androgen stimulates AR translocation to cell nuclei hence blocks its binding DNA and shuts down the downstream oncogenic signaling. Moreover, GT0918 induces AR down regulation in prostate cancer cells. GT0918 not only inhibits proliferation of hormone-sensitive CaP cells, but also more potently inhibits proliferation of CRPC cells. In addition, GT0918 inhibits the growth of AR positive breast cancer cells. In contrast, GT0918 has minimum effects on the growth of AR-negative CaP cells (PC-3 and DU145), indicating it is a selective AR pathway inhibitor[1].

In Vivo

The major pharmacokinetic parameters and statistical moment parameters are summarized. 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. Moreover, the difference between the tmax of the two treatments is statistically significant (p<0.05). The mean Cmaxand 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. 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 mean 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 pharmacoki-netic theory: the extent and rate of absorption should not affect elimination[2].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

Beagle Dogs[2]
A single dose (25 mg GT0918), 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

517.50

Formula

C₂₄H₁₉F₄N₅O₂S

CAS No.

1398046-21-3

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Proxalutamide
Cat. No.:
HY-103184
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Proxalutamide

Cat. No.: HY-103184