Name: Galeterone
Brand: Selleck Chemicals
SKU: S2803
Rating: 5 (6 reviews)

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	Adrenergic Receptor Estrogen/progestogen Receptor GPR Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR
Other Androgen Receptor Inhibitors	Bavdegalutamide (ARV-110) RU58841 EPI-001 Cyproterone Acetate 3,3'-Diindolylmethane Ailanthone Proxalutamide (GT0918) AZD3514 Chlormadinone acetate ORM-15341

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description
human PC3 cells	Function assay			Displacement of [3H]R1881 from androgen receptor in human PC3 cells, EC50=0.405 μM
human LNCaP cells	Function assay		2 h	Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis, EC50=0.67 μM
human CWR22Rv1 cells	Function assay			Induction of apoptosis in human CWR22Rv1 cells assessed as induction of PARP cleavage
human LNCAP cells	Function assay	5 μM	48 h	Down regulation of AR protein expression in human LNCAP cells at 5 uM after 48 hrs by DAPI staining-based immunocytochemical analysis
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	388.55	Formula	C₂₆H₃₂N₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	851983-85-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	TOK-001			Smiles	CC12CCC(CC1=CCC3C2CCC4(C3CC=C4N5C=NC6=CC=CC=C65)C)O

Solubility

In vitro
Batch:

Ethanol : 40 mg/mL

DMSO : 24 mg/mL (61.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	0.5% hydroxyethyl cellulose Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (25.74mM)	Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% hydroxyethyl cellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	CYP17 (Cell-free assay) 300 nM Androgen Receptor (PC3AR) 384 nM
In vitro	Galeterone is effective at preventing binding of [³H]-R1881 to the mutant LNCaP AR (T877A) with IC50 of 845 nM. This compound inhibits the DHT-induced proliferation of LNCaP and LAPC4 cells in a dose-dependent manner with IC50 of 6 μM and 3.2 μM, respectively. It also inhibits the binding of [³H]-R1881 to the T575A mutant AR in PC3 cells with IC50 of 454 nM. This chemical potently inhibits the proliferation of LNCaP and LAPC4 cells in the absence of DHT stimulation with IC50 of 2.6 μM and 4 μM, respectively. Furthermore, this compound treatment increases the degradation rate of the AR in a dose-dependent manner. It potently inhibits the growth of the androgen-independent cell lines PC-3 and DU-145 in a dose-dependent manner with GI50 of 7.82 μM and 7.55 μM, respectively. This chemical induces the endoplasmic reticulum stress response resulting in down-regulation of cyclin D1 protein expression and cyclin E2 mRNA. It effectively inhibits proliferation of HP-LNCaP and C4-2B cell lines with IC50 of 2.9 μM and 9.7 μM, respectively. This compound treatment at 1 μM effectively inhibits Androgen Receptor activation in LNCaP cells (50%) and HP-LNCaP cells (70%). It decreases activation of the Androgen Receptor in both LNCaP cells and HP-LNCaP cells with IC50 of 1 μM and 411 nM, respectively, and down-regulates Androgen Receptor protein expression by 50% after 24 hour of treatment. This chemical reduces AR protein and mRNA expression, antagonises AR-dependent promoter activation induced by androgen, and significantly reduces the phospho-4EBP1 levels.
Kinase Assay	In vitro assay of CYP17
Kinase Assay	The in vitro CYP17 inhibitory activity of Galeterone is evaluated using rapid acetic acid releasing assay (AARA), utilising intact P450c17-expressing E. coli as the enzyme source. It involves the use of [21-³H]-17 -hydroxypregnenolone as the substrate, and CYP17 activity is measured by the amount of tritiated acetic acid formed during the cleavage of the C-21 side chain of the substrate. IC50 value is obtained directly from plots relating percentage inhibition versus this compound concentration over appropriate ranges.
In vivo	Administration of Galeterone at 50 mg/kg twice daily is very effective at inhibiting the growth of androgen-dependent LAPC4 human prostate tumour xenograft, with a 93.8% reduction in the mean final tumour volume compared with controls, and it is also significantly more effective than castration. Treatment of this compound (0.13 mM/kg twice daily) or this compound (0.13 mmol/kg twice daily) plus castration induces regression of LAPC4 tumour xenografts in SCID mice by 26.55% and 60.67%, respectively. Treatments with this compound or this compound plus castration causes marked reduction in AR protein of 10- and 5-fold, respectively.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15828836/ [2] https://pubmed.ncbi.nlm.nih.gov/18723482/ [3] https://pubmed.ncbi.nlm.nih.gov/18790763/ [4] https://pubmed.ncbi.nlm.nih.gov/18202015/ [5] https://pubmed.ncbi.nlm.nih.gov/20842117/ [6] https://pubmed.ncbi.nlm.nih.gov/22174412/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02729376	Completed	Healthy	LTN PHARMACEUTICALS INC.	March 2016	Phase 1

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Galeterone Androgen Receptor antagonist

Chemical Structure

Molecular Weight: 388.55