Proxalutamide (GT0918)

Catalog No.S9898 Batch:S989801

Technical Data

Formula	C₂₄H₁₉F₄N₅O₂S
Molecular Weight	517.50	CAS No.	1398046-21-3
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (193.23 mM)
		Ethanol	25 mg/mL (48.3 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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.

Targets

Androgen Receptor ^[1]
(in the AR competive binding assay)

32 nM

In vitro

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]

In vivo

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]

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[2]}	Animal Models Sprague–Dawley rats Dosages 20 mg/kg Administration o.g., i.v.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[2]}

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

References

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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