Cat. No.: HY-70006

Galeterone

(Synonyms: TOK-001; VN-124-1)

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

Galeterone (TOK-001) is a potent, orally active molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. Galeterone also functions as a CYP17 inhibitor (IC₅₀ = 47 nM). Galeterone induces cell apoptosis. Galeterone inhibits tumor growth in human prostate cancer xenograft mouse models. Galeterone can be used for castration resistant prostate cancer (CRPC) and pancreatic ductal adenocarcinoma (PDAC) research^[1][2].

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Pureté: 99.87%
CAS No.: 851983-85-2
Formule: C₂₆H₃₂N₂O
Masse moléculaire:388.55

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Galeterone Chemical Structure

CAS No.: 851983-85-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (3)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

CYP17

47 nM (IC₅₀)

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Cellular Effect

Cell Line	Type	Value	Description	References
A549	GI₅₀	3.9 μM Compound: Galeterone	Antiproliferative activity against human A549 cells after 48 hrs by SRB assay Antiproliferative activity against human A549 cells after 48 hrs by SRB assay	[PMID: 29172080]
Cancer cell lines	IC₅₀	2.9 μM Compound: 33, VN/124-1, galeterone, TOK-001	Growth inhibition of human castration-resistant prostate cancer cells Growth inhibition of human castration-resistant prostate cancer cells	[PMID: 25591066]
CWR22R	GI₅₀	37.8 μM Compound: Galeterone	Antiproliferative activity against AR-positive human 22Rv1 cells harboring ARE14 construct assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against AR-positive human 22Rv1 cells harboring ARE14 construct assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay	[PMID: 31271960]
CWR22R	IC₅₀	11.6 μM Compound: Galeterone	Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 38512060]
CWR22R	IC₅₀	8.91 μM Compound: 5; Galeterone	Antiproliferative activity against human CWR22Rv1 cells after 7 days by MTT assay Antiproliferative activity against human CWR22Rv1 cells after 7 days by MTT assay	[PMID: 27437082]
HBL-100	GI₅₀	10 μM Compound: Galeterone	Antiproliferative activity against human HBL100 cells after 48 hrs by SRB assay Antiproliferative activity against human HBL100 cells after 48 hrs by SRB assay	[PMID: 29172080]
HeLa	GI₅₀	5.3 μM Compound: Galeterone	Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay Antiproliferative activity against human HeLa cells after 48 hrs by SRB assay	[PMID: 29172080]
hTERT-BJ	GI₅₀	5 μM Compound: Galeterone	Cytotoxicity against human hTERT-BJ cells assessed as cell growth inhibition after 48 hrs SRB assay Cytotoxicity against human hTERT-BJ cells assessed as cell growth inhibition after 48 hrs SRB assay	[PMID: 29172080]
L02	IC₅₀	>100 μM Compound: Galeterone	Antiproliferative activity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human L02 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 38512060]
LNCaP	EC₅₀	670 nM Compound: 5, TOK-001, Galeterone	Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis	[PMID: 23713567]
LNCaP	EC₅₀	845 nM Compound: 33, VN/124-1, galeterone, TOK-001	Displacement of [3H]R1881 from androgen receptor in human LNCAP cells Displacement of [3H]R1881 from androgen receptor in human LNCAP cells	[PMID: 25591066]
LNCaP	GI₅₀	3.35 μM Compound: 5, TOK-001, Galeterone	Cytotoxicity against human LNCAP cells after 7 days by MTT assay Cytotoxicity against human LNCAP cells after 7 days by MTT assay	[PMID: 23713567]
LNCaP	IC₅₀	2 μM Compound: Galeterone	Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against human LNCaP cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 38512060]
LNCaP	IC₅₀	3.93 μM Compound: 5; Galeterone	Antiproliferative activity against human LNCAP cells after 7 days by MTT assay Antiproliferative activity against human LNCAP cells after 7 days by MTT assay	[PMID: 27437082]
LNCaP	IC₅₀	3548 nM Compound: 6; TOK-001, VN/124-1	Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability measured after 6 days by CellTiter-Glo assay Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability measured after 6 days by CellTiter-Glo assay	[PMID: 36070471]
LNCaP C4-2	GI₅₀	>40 μM Compound: Galeterone	Antiproliferative activity against AR-positive human C4-2 cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against AR-positive human C4-2 cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay	[PMID: 31271960]
PC-3	EC₅₀	405 nM Compound: 33, VN/124-1, galeterone, TOK-001	Displacement of [3H]R1881 from androgen receptor in human PC3 cells Displacement of [3H]R1881 from androgen receptor in human PC3 cells	[PMID: 25591066]
PC-3	GI₅₀	37.7 μM Compound: Galeterone	Antiproliferative activity against AR-negative human PC3 cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against AR-negative human PC3 cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay	[PMID: 31271960]
SW1573	GI₅₀	3.9 μM Compound: Galeterone	Antiproliferative activity against human SW1573 cells after 48 hrs by SRB assay Antiproliferative activity against human SW1573 cells after 48 hrs by SRB assay	[PMID: 29172080]
T47D	GI₅₀	2.1 μM Compound: Galeterone	Antiproliferative activity against human T47D cells after 48 hrs by SRB assay Antiproliferative activity against human T47D cells after 48 hrs by SRB assay	[PMID: 29172080]
VCaP	GI₅₀	>40 μM Compound: Galeterone	Antiproliferative activity against AR-positive human VCaP cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against AR-positive human VCaP cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay	[PMID: 31271960]
WiDr	GI₅₀	2.7 μM Compound: Galeterone	Antiproliferative activity against human WiDr cells after 48 hrs by SRB assay Antiproliferative activity against human WiDr cells after 48 hrs by SRB assay	[PMID: 29172080]

In Vitro

Galeterone (compound 1) possess potent antiproliferative activities with GI₅₀ of 2.43 μM, 2.20 μM, 3.80 μM against LNCaP (androgen-sensitive), C42B (androgen-insensitive) and CWR22Rv1 (castration-resistant), respectively^[1].
Galeterone (5-20 μM; 24 h) can degrade AR/AR-V7 and Mnk1/2 with consequent inhibition of AR signaling and depletion of peIF4E, respectively, and modulation of the downstream molecular targets in human CWR22Rv1 prostate cancer cell^[1].
Galeterone (compound 5) (1-15 μM, 24 h) causes AR down-regulation in LNCaP cells, with nearly complete (>95%) AR down-regulation at 15 μM^[2].

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

Western Blot Analysis^[1]

Cell Line:

CWR22Rv1 prostate cancer cells
Concentration:

5, 10 and 20 μM
Incubation Time:

24 h
Result:

Significantly and dose-dependently reduced the expressions of Mnk1, and peIF4E.
Caused significant depletion of the downstream target, cyclin D1, and induction of apoptosis via significant downregulation of antiapoptotic Bcl-2 and upregulation of proapoptotic Bax.

Western Blot Analysis^[2]

Cell Line:

LNCaP cells
Concentration:

1, 5, 10 and 15 μM
Incubation Time:

24 h
Result:

Almost completed AR down-regulation at 15 μM.

In Vivo

Galeterone (compound 1) (100 mg/kg; p.o.; b.i.d.; 5 days per/week; for 16 days) shows antitumor activity in CWR22Rv1 tumor xenograft^[1].
Galeterone (compound 5) (0.15 mmol/kg; s.c.; b.i.d. for 31 days) shows antitumor activity in a LAPC-4 xenograft mouse model^[2].

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

Animal Model:

Male NRG mice (5-6 weeks) bearing CWR22Rv1 tumors^[1]
Dosage:

100 mg/kg
Administration:

p.o.; b.i.d.; 5 days per/week; for 16 days
Result:

Exhibited statistically significant robust inhibition of CWR22Rv1 tumor growth at the tested doses.
Inhibited tumor growth with a TGI of 64%.

Animal Model:

Male SCID mice (4-6 weeks) subcutaneously injected with LAPC-4 tumors^[2]
Dosage:

0.15 mmol/kg
Administration:

s.c.; b.i.d. for 31 days
Result:

Significantly reduced the growth rate of tumor growth compared to control.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 851983-85-2
Appearance Solid
Masse moléculaire 388.55
Formule C₂₆H₃₂N₂O
Color White to off-white
SMILES

C[C@@]12C(N3C=NC4=CC=CC=C34)=CC[C@]1([C@@]5(CC=C6[C@@](C)([C@]5(CC2)[H])CC[C@@H](C6)O)[H])[H]
Synonyms

TOK-001; VN-124-1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Nature

Structures of cytochrome P450 17A1 with prostate cancer drugs abiraterone and TOK-001. [Abstract]

2012 Jan 22;482(7383):116-9. PMID: 22266943
Drug Metab Dispos

Structural and Functional Evaluation of Clinically Relevant Inhibitors of Steroidogenic Cytochrome P450 17A1. [Abstract]

2017 Jun;45(6):635-645. PMID: 28373265
Patent

US20240400606A1.

Solvant et solubilité

In Vitro:

DMSO : 25 mg/mL (64.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5737 mL

12.8684 mL

25.7367 mL

5 mM

0.5147 mL

2.5737 mL

5.1473 mL

10 mM

0.2574 mL

1.2868 mL

2.5737 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (282 KB)
SDS (419 KB)
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Elemental Analysis Report (2659 KB)
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Références

[1]. Thankan RS, et al. Salinization Dramatically Enhance the Anti-Prostate Cancer Efficacies of AR/AR-V7 and Mnk1/2 Molecular Glue Degraders, Galeterone and VNPP433-3β Which Outperform Docetaxel and Enzalutamide in CRPC CWR22Rv1 Xenograft Mouse Model. Bioorg Chem. 2023 Oct;139:106700. [Content Brief]

[2]. Bruno RD, et al. Synthesis and biological evaluations of putative metabolically stable analogs of VN/124-1 (TOK-001): head to head anti-tumor efficacy evaluation of VN/124-1 (TOK-001) and abiraterone in LAPC-4 human prostate cancer xenograft model.Steroid [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5737 mL	12.8684 mL	25.7367 mL	64.3418 mL
	5 mM	0.5147 mL	2.5737 mL	5.1473 mL	12.8684 mL
	10 mM	0.2574 mL	1.2868 mL	2.5737 mL	6.4342 mL
	15 mM	0.1716 mL	0.8579 mL	1.7158 mL	4.2895 mL
	20 mM	0.1287 mL	0.6434 mL	1.2868 mL	3.2171 mL
	25 mM	0.1029 mL	0.5147 mL	1.0295 mL	2.5737 mL
	30 mM	0.0858 mL	0.4289 mL	0.8579 mL	2.1447 mL
	40 mM	0.0643 mL	0.3217 mL	0.6434 mL	1.6085 mL
	50 mM	0.0515 mL	0.2574 mL	0.5147 mL	1.2868 mL
	60 mM	0.0429 mL	0.2145 mL	0.4289 mL	1.0724 mL

Galeterone

3 Cited Publications

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Galeterone

Antioxidant Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Anti-Pancreatic Cancer Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Protein-protein Interaction Inhibitor Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Molecular Glue Compound Library

Metabolic Enzyme Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

MAPK Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Galeterone

Voir tous les produits spécifiques à Isoform MNK

Voir tous les produits spécifiques à Isoform Cytochrome P450

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Galeterone Related Classifications

HY-70006 Related Classifications