Art. -Nr.: HY-14250

PF-998425

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PF-998425 is a potent, selective nonsteroidal androgen receptor (AR) antagonist with an IC₅₀ of 37 nM and 43 nM in AR binding and cellular assays, respectively. PF-998425 has low activity on common receptors and enzymes, such as progesterone receptor. PF-998425 can be used for sebum control and androgenetic alopecia research.

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Reinheit: 98.63%
CAS. Nr.: 1076225-27-8
Formel: C₁₄H₁₄F₃NO
Molecular Weight:269.26

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PF-998425 Chemical Structure

CAS. Nr.: 1076225-27-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 37 nM (AR binding) and 43 nM (AR cellular)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-453	IC₅₀	43 nM Compound: (-)-6a, PF-0998425	Antagonist activity against human androgen receptor expressed in human MDA-MB-453 cells assessed as inhibition of dihydrotestosterone-induced effect by luciferase receptor gene assay Antagonist activity against human androgen receptor expressed in human MDA-MB-453 cells assessed as inhibition of dihydrotestosterone-induced effect by luciferase receptor gene assay	[PMID: 18921992]
Sf9	IC₅₀	37 nM Compound: (-)-6a, PF-0998425	Displacement of [3H]dihydrotestosterone from human androgen receptor expressed in Sf9 cells Displacement of [3H]dihydrotestosterone from human androgen receptor expressed in Sf9 cells	[PMID: 18921992]

In Vivo

PF-998425 (Compound (-)-6a) is rapidly metabolized in rat liver microsomes (t_1/2=4 min, C_Lint=350 (µL/min)/mg protein). In vivo clearance data in dogs are consistent with the high clearance predicted in vitro in rat. Following intravenous administration of PF-998425, mean systemic plasma clearance is 40 (mL/min)/kg. The mean apparent of volume of distribution at steady state is 6.5 L/kg, and the mean terminal phase half-life is 2.6 h^[1].

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

Chemical Information

CAS. Nr. 1076225-27-8
Appearance Solid
Molecular Weight 269.26
Formel C₁₄H₁₄F₃NO
Color White to off-white
SMILES

O[C@H]1[C@H](CCCC1)C2=CC(C(F)(F)F)=C(C=C2)C#N
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (185.69 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

3.7139 mL

18.5694 mL

37.1388 mL

5 mM

0.7428 mL

3.7139 mL

7.4278 mL

10 mM

0.3714 mL

1.8569 mL

3.7139 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, 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 (9.28 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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 (9.28 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 (9.28 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Jie Jack Li, et al. Rational design and synthesis of 4-((1R,2R)-2-hydroxycyclohexyl)-2(trifluoromethyl)benzonitrile (PF-998425), a novel, nonsteroidal androgen receptor antagonist devoid of phototoxicity for dermatological indications. J Med Chem. 2008 Nov 13;51(21):7010-4. [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, 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	3.7139 mL	18.5694 mL	37.1388 mL	92.8471 mL
	5 mM	0.7428 mL	3.7139 mL	7.4278 mL	18.5694 mL
	10 mM	0.3714 mL	1.8569 mL	3.7139 mL	9.2847 mL
	15 mM	0.2476 mL	1.2380 mL	2.4759 mL	6.1898 mL
	20 mM	0.1857 mL	0.9285 mL	1.8569 mL	4.6424 mL
	25 mM	0.1486 mL	0.7428 mL	1.4856 mL	3.7139 mL
	30 mM	0.1238 mL	0.6190 mL	1.2380 mL	3.0949 mL
	40 mM	0.0928 mL	0.4642 mL	0.9285 mL	2.3212 mL
	50 mM	0.0743 mL	0.3714 mL	0.7428 mL	1.8569 mL
	60 mM	0.0619 mL	0.3095 mL	0.6190 mL	1.5475 mL
	80 mM	0.0464 mL	0.2321 mL	0.4642 mL	1.1606 mL
	100 mM	0.0371 mL	0.1857 mL	0.3714 mL	0.9285 mL

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PF-998425

Endocrinology Compound Library

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-998425

Endocrinology Compound Library

Transcription Factor-Targeted Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-998425 Related Classifications

HY-14250 Related Classifications