2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. Galeterone

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

Cat. No.: HY-70006 Purity: 99.87%
COA Handling Instructions

Molarity Calculator

Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).

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

Galeterone Chemical Structure

Galeterone Chemical Structure

CAS No. : 851983-85-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
1 mg USD 26 In-stock
5 mg USD 66 In-stock
10 mg USD 99 In-stock
50 mg USD 297 In-stock
100 mg USD 495 In-stock
200 mg USD 715 In-stock
500 mg USD 1265 In-stock
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5 g   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Galeterone Related Antibodies

Top Publications Citing Use of Products

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).

IC50 & Target

CYP17

 

In Vitro

Galeterone (TOK-001) affords strong CYP17 lyase inhibition, with IC50 of 47 nM[1]. Galeterone (TOK-001) is both a CYP17A1 inhibitor and androgen receptor antagonist and the similarity of these binding modes is likely the reason for this dual mechanism of action.This CYP17A1 binds abiraterone and Galeterone (TOK-001) with absorbance decreases at 402 nm and increases at 424 nm, consistent with nitrogen binding to the heme iron (type II interaction) with Kd of <100 nM[2]. When LNCaP cells are cultured in medium supplemented with charcoal-stripped serum (CSS, T<1 nM) followed by treatment with increasing concentrations of Galeterone (TOK-001), the steady-state levels of AR protein are markedly decreased (up to 84%, 15 μM Galeterone (TOK-001)). In LAPC-4 cells, abiraterone alcohol reduced AR expression to a greater extent than Galeterone (TOK-001) at concentrations greater than or equal to 1 μM. When LNCaP cells are treated with 20 μM TOK-001 for 24 h, AR mRNA levels are reduced by 38%[3].

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

Galeterone Related Antibodies
In Vivo

Mice inoculated with LAPC-4 tumors are treated subcutaneously with 0.15 mmol/kg of Galeterone (TOK-001) twice daily. Mice treated with TOK-001 have smaller average tumor volume on day 31 when compared to control (p= 0.0001). Galeterone (TOK-001) treatment also significantly reduces the growth rate of tumor growth compared to control (p<0.0001). Upon excision, final tumor weights are also significantly reduced in animals treated with Galeterone (TOK-001) compared to animals treated with control, and castration (p<0.05)[1].

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

388.55

Formula

C26H32N2O
CAS No.
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
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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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%

COA (252 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[3]

LNCaP cells are seeded in 24-well plates at 70% confluence a day before transfections. Cells then are transfected with plasmid DNA (0.5 μg/well) carrying pIR-AR 5′UTR-Luc (5′UTR; test) or pIRES-Luc (IRES, control) for 6 h in serum-free and antibiotic-free conditions. Transcription of both luciferase reporter genes is under the control of the CMV promoter. Lipofectamine 2000 reagent is used in all transfections according to the manufacturer's instructions. Cells are then treated with doses of Galeterone (TOK-001) (0, 10, and 20 μM) in 5% FBS/T-Medium. Luciferase reporter gene activities are measured using Luciferase Assay System from Promega at 36 h post treatment using a BMG Labtech microplate reader. Relative luciferase units are normalized to total protein and then normalized to vector control (pIR-AR 5′UTR-Luc) and the result is presented as luciferase activity. For cell proliferation studies, LNCaP cells in 96-well plate are seeded 24 h prior to drug treatment and then treated with control (mock), Galeterone (TOK-001) (10 μM), or abiraterone alcohol (10 μM) in 5% FBS/T-medium for 72 h. Cell proliferation is determined using MTS[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Mice inoculated with LAPC-4 tumors are treated subcutaneously with 0.15 mmol/kg of Galeterone (TOK-001) twice daily. Mice treated with TOK-001 have smaller average tumor volume on day 31 when compared to control (p=0.0001). Galeterone (TOK-001) treatment also significantly reduced the growth rate of tumor growth compared to control (p<0.0001). Upon excision, final tumor weights are also significantly reduced in animals treated with Galeterone (TOK-001) compared to animals treated with control, and castration (p<0.05).

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

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.

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
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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.

Keywords:

Galeterone851983-85-2TOK-001 VN-124-1TOK001TOK 001Cytochrome P450CYPsInhibitorinhibitorinhibit

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