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

Name: Galeterone
Brand: MedChemExpress
SKU: HY-70006
Rating: 5.0 (3 reviews)

Cat. No.: HY-70006 Purity: 99.87%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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].

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

Galeterone Chemical Structure

CAS No. : 851983-85-2

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	Get quote
5 g	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Galeterone:

Galeterone hydrochloride Get quote

3 Publications Citing Use of MCE Galeterone

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All MNK Isoform Specific Products:

View All Isoforms

MNK1 MNK2 MNK

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms

CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

CYP17

47 nM (IC₅₀)

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]
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]
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]
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]
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]
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]

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.

Clinical Trial

Molecular Weight

388.55

Formula

C₂₆H₃₂N₂O

CAS No.

851983-85-2

Appearance

Solid

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]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.87%

Select Batch:

Data Sheet (282 KB) SDS (419 KB)

COA (252 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Please select a local distributor ナミキ商事株式会社コスモ・バイオ株式会社重松貿易株式会社
Product Name			Requested Quantity *
Applicant Name *			Salutation
Email Address *			Phone Number *
Department			Organization Name *
City			State
Country or Region *
Remarks

Product Name			Lot #
Applicant Name *			Email Address *
Phone Number			Department *
Organization Name *			Country or Region *
Remarks

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

Customer Review

Other Forms of Galeterone:

3 Publications Citing Use of MCE Galeterone

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All MNK Isoform Specific Products:

View All Cytochrome P450 Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Galeterone Related Classifications

Keywords:

Your Recently Viewed Products:

Name
Email *

	Sorry, but the email address you supplied was invalid.

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

Customer Review

Other Forms of Galeterone:

Galeterone Related Antibodies

3 Publications Citing Use of MCE Galeterone

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All MNK Isoform Specific Products:

View All Cytochrome P450 Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Galeterone Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Galeterone Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report