Home Endocrinology & Hormones Androgen Receptor antagonist Proxalutamide (GT0918) For research use only.

Proxalutamide (GT0918)

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.

Proxalutamide (GT0918) Chemical Structure

Proxalutamide (GT0918) Chemical Structure

CAS No. 1398046-21-3

Purity & Quality Control

Batch: S989801 DMSO]100 mg/mL]false]Ethanol]25 mg/mL]false]Water]Insoluble]false Purity: 98.95%
98.95

Proxalutamide (GT0918) Related Products

Signaling Pathway

Androgen Receptor Signaling Pathways

Androgen Receptor Signaling Pathway

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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Sprague–Dawley rats
Dosages 20 mg/kg
Administration o.g., i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04870606 Completed
Efficacy and Safety
Suzhou Kintor Pharmaceutical Inc
 March 5 2021 Phase 3
NCT03899467 Completed
Metastatic Castrate Resistant Prostate Cancer (mCRPC)|Metastatic Hormone-Sensitive Prostate Cancer (mHSPC)
Suzhou Kintor Pharmaceutical Inc
 May 30 2019 Phase 2

Chemical Information & Solubility

Molecular Weight 517.50 Formula

C24H19F4N5O2S
CAS No. 1398046-21-3 SDF --
Smiles CC1(C)N(C(=S)N(C1=O)C2=C(F)C(=C(C=C2)C#N)C(F)(F)F)C3=CN=C(CCCC4=NC=CO4)C=C3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (193.23 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 25 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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