1. Metabolic Enzyme/Protease
  2. Drug Metabolite
  3. Enzalutamide carboxylic acid

Enzalutamide carboxylic acid  (Synonyms: MDV3100 carboxylic acid)

Cat. No.: HY-70002B Purity: 98.11%
COA Handling Instructions

Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist.

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

Enzalutamide carboxylic acid Chemical Structure

Enzalutamide carboxylic acid Chemical Structure

CAS No. : 1242137-15-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 176 In-stock
Solution
10 mM * 1 mL in DMSO USD 176 In-stock
Solid
1 mg USD 76 In-stock
5 mg USD 160 In-stock
10 mg USD 250 In-stock
50 mg USD 560 In-stock
100 mg USD 850 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Enzalutamide carboxylic acid:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Enzalutamide carboxylic acid

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist[1].

In Vitro

Enzalutamide is converted into its major metabolites, N-desmethyl enzalutamide and carboxylic acid enzalutamide, by cytochrome P450 (CYP) 3A4/5 and CYP2C8, respectively. N-desmethyl enzalutamide has clinically relevant anti-androgen capacities similar to enzalutamide, whereas carboxylic acid enzalutamide is inactive[1].

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

Molecular Weight

451.39

Formula

C20H13F4N3O3S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=C(N(C(N2C3=CC=C(C#N)C(C(F)(F)F)=C3)=S)C(C)(C)C2=O)C=C1F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (276.92 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 2.2154 mL 11.0769 mL 22.1538 mL
5 mM 0.4431 mL 2.2154 mL 4.4308 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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: ≥ 2.08 mg/mL (4.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2154 mL 11.0769 mL 22.1538 mL 55.3845 mL
5 mM 0.4431 mL 2.2154 mL 4.4308 mL 11.0769 mL
10 mM 0.2215 mL 1.1077 mL 2.2154 mL 5.5384 mL
15 mM 0.1477 mL 0.7385 mL 1.4769 mL 3.6923 mL
20 mM 0.1108 mL 0.5538 mL 1.1077 mL 2.7692 mL
25 mM 0.0886 mL 0.4431 mL 0.8862 mL 2.2154 mL
30 mM 0.0738 mL 0.3692 mL 0.7385 mL 1.8461 mL
40 mM 0.0554 mL 0.2769 mL 0.5538 mL 1.3846 mL
50 mM 0.0443 mL 0.2215 mL 0.4431 mL 1.1077 mL
60 mM 0.0369 mL 0.1846 mL 0.3692 mL 0.9231 mL
80 mM 0.0277 mL 0.1385 mL 0.2769 mL 0.6923 mL
100 mM 0.0222 mL 0.1108 mL 0.2215 mL 0.5538 mL
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Enzalutamide carboxylic acid 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.

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Enzalutamide carboxylic acid
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