2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. Apalutamide

Apalutamide  (Synonyms: ARN-509)

Cat. No.: HY-16060 Purity: 99.93%
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Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.

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

Apalutamide Chemical Structure

Apalutamide Chemical Structure

CAS No. : 956104-40-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 204 In-stock
Solution
10 mM * 1 mL in DMSO USD 204 In-stock
Solid
5 mg USD 119 In-stock
10 mg USD 185 In-stock
50 mg USD 550 In-stock
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Based on 11 publication(s) in Google Scholar

Other Forms of Apalutamide:

Apalutamide Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

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Description

Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM[1].

IC50 & Target

IC50: 16 nM (Androgen receptor)[1]
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.016 μM
Compound: 6
Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay
Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay
[PMID: 30525603]
LNCaP IC50
174 nM
Compound: 5, ARN-509
Antiproliferative activity against human LNCAP cells after 3 days
Antiproliferative activity against human LNCAP cells after 3 days
[PMID: 26046313]
In Vitro

Apalutamide (ARN-509) also exhibits low micromolar affinity (IC50 3 μM) for the GABAA receptor in radioligand binding-assays and thus may potentially antagonize GABAA at therapeutic dose levels[1]. Apalutamide is a potent androgen receptor (AR) antagonist that targets the AR ligand-binding domain and prevents AR nuclear translocation, DNA binding, and transcription of AR gene targets[2].

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

Apalutamide Related Antibodies
In Vivo

Apalutamide (ARN-509) exhibits low systemic clearance, high oral bioavailability and long plasma half-life in both mouse and dog, supporting once-daily oral dosing. Consistent with its long terminal-half-life, Apalutamide steady-state plasma-levels increases in repeat-dose studies, resulting in high C24hr levels and low peak:trough ratios (ratio:2.5). Castrate male mice bearing LNCaP/AR xenograft tumors are treated with either Apalutamide at doses of 1, 10 or 30 mg/kg/day. Thirteen of 20 Apalutamide (30 mg/kg/day)-treated animals exhibit >50% reduction in tumor-volume at day 28 versus 3 of 19 MDV3100 (30 mg/kg/day)-treated mice[1].

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

477.43

Formula

C21H15F4N5O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC)C1=CC=C(N(C(N(C2=CC(C(F)(F)F)=C(C#N)N=C2)C3=O)=S)C43CCC4)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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (104.73 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 2.0945 mL 10.4727 mL 20.9455 mL
5 mM 0.4189 mL 2.0945 mL 4.1891 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.

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  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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 (4.36 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 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)

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: 99.93%

SDS (393 KB)

COA (252 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

Trypsinized VCaP cells are adjusted to a concentration of 100,000 cells per mL in phenol-red-free RPMI 1640 (with 5% CSS), and dispensed in 16 µL aliquots into CellBIND 384 well plates. Cells are incubated for 48 hours, after which ligand is added in a 16 µL volume to the RPMI culture medium. For the antagonist mode assay, the ligands are diluted in culture medium also containing 30 pM R1881. After 7 days’ incubation, 16 µL of CellTiter-Glo Luminescent Cell Viability Assay is added and Relative Luminescence Units (RLUs) measured[1].

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

Mice[1]
In vivo xenograft experiments to determine anti-tumor response are carried out in SHO SCID male mice. Mice are orchiectomized under isoflorane anesthesia and are given 2-3 days to recover prior to tumor cell injection. LNCaP/AR(cs) cells are suspended in 50% RPMI, 50% Matrigel, and 5×106 cells/xenograft are injected in a volume of 100 μL. Animals are observed weekly until tumor growth is apparent. From 24 d post-injection, tumors are measured weekly, and after 40-60 days post-injection, animals are randomized into cohorts of equivalent mean (150-250 mm3) and range tumor burden. All compounds (e.g., Apalutamide, 30 mg/kg per day) are administered daily by oral gavage. Statistical analyses are performed using Graphpad Prism.

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 2.0945 mL 10.4727 mL 20.9455 mL 52.3637 mL
5 mM 0.4189 mL 2.0945 mL 4.1891 mL 10.4727 mL
10 mM 0.2095 mL 1.0473 mL 2.0945 mL 5.2364 mL
15 mM 0.1396 mL 0.6982 mL 1.3964 mL 3.4909 mL
20 mM 0.1047 mL 0.5236 mL 1.0473 mL 2.6182 mL
25 mM 0.0838 mL 0.4189 mL 0.8378 mL 2.0945 mL
30 mM 0.0698 mL 0.3491 mL 0.6982 mL 1.7455 mL
40 mM 0.0524 mL 0.2618 mL 0.5236 mL 1.3091 mL
50 mM 0.0419 mL 0.2095 mL 0.4189 mL 1.0473 mL
60 mM 0.0349 mL 0.1745 mL 0.3491 mL 0.8727 mL
80 mM 0.0262 mL 0.1309 mL 0.2618 mL 0.6545 mL
100 mM 0.0209 mL 0.1047 mL 0.2095 mL 0.5236 mL
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Apalutamide 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:

Apalutamide956104-40-8ARN-509ARN509ARN 509Androgen ReceptorInhibitorinhibitorinhibit

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