1. Others
    Anti-infection
  2. Androgen Receptor
    SARS-CoV
  3. Proxalutamide

Proxalutamide (Synonyms: GT0918; Pruxelutamide)

Cat. No.: HY-103184 Purity: 98.79%
Handling Instructions

Proxalutamide (GT0918) is an orally active potent androgen receptor (AR) antagonist. Proxalutamide (GT0918) can be used in the study for prostate cancer and COVID-19.

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

Proxalutamide Chemical Structure

Proxalutamide Chemical Structure

CAS No. : 1398046-21-3

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 569 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 569 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 500 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3000 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Proxalutamide (GT0918) is an orally active potent androgen receptor (AR) antagonist. Proxalutamide (GT0918) can be used in the study for prostate cancer and COVID-19[1][2][3][4][5].

IC50 & Target

Androgen Receptor[1].

In Vitro

Proxalutamide (GT0918) down-regulates AR protein level in prostate cancer cells[1].
Proxalutamide can overcome the resistance of prostatic cancer cells by downregulating the expression of AR genes[4].
Proxalutamide (GT0918, 0-200 μM) dose-dependently inhibits cell viability in LNCaP and 22RV1[5].

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

Cell Viability Assay[5].

Cell Line: Four human PCa cell lines, LNCaP, 22RV1, PC3 and DU145.
Concentration: 1, 2, 5, 10, 20, 50, 100, and 200 μM.
Incubation Time: Up to 72 h.
Result: Preferentially affected AR-positive PCa cells (IC50 values from 6.90 to 32.07 μM) over AR-negative cells (IC50 > 200 μM).
In Vivo

The elimination half-life (t1/2) 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 (Cmax) could reach 2 μg/mL or higher, and the oral absolute bioavailability (F) was approximately 80%[4].

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

Animal Model: Rats[4].
Dosage: 20 mg/kg (Pharmacokinetic Analysis).
Administration: Intragastrically.
Result: T1/2 = 2 h and F% = 80%
Clinical Trial
Molecular Weight

517.50

Formula

C24H19F4N5O2S

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (193.24 mM; Need ultrasonic)

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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (4.83 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.83 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: 98.79%

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