PF-02413873
Based on 1 Customer Validation
PF-02413873 (PF-2413873) is a potent selective, fully competitive and orally active nonsteroidal progesterone receptor (PR) antagonist, with a Ki of 2.6 nM. PF-02413873 can block progesterone binding and PR nuclear translocation, and inhibit endometrial growth in vivo.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.88%
- No. CAS: 936345-35-6
- Fòrmula: C18H21N3O3S
- Peso molecular:359.44
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Ki: 2.6 nM (progesterone receptor)[1]
PF-02413873 shows potent PR antagonist activity with a derived Ki of 9.7 nM in the T47D native functional assay[1].
PF-02413873 (1 nM-10 μM) induces nuclear translocation only at high concentrations (>3 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PF-02413873 (3 mg/kg; a single p.o.) exhibits t1/2 (4.2 h), Cmax (162 ng/mL) and CL/F (41 mL/min/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cynomolgus macaques (3.7-5.7 kg; 5-6 years)[1]
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Dosage:2.5, 10 mg/kg
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Administration:P.o. twice daily for 10 days
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Result:Reduced the endometrial thickness of 43 and 56% at the dose of 2.5 and 10 mg/kg, respectively.
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Animal Model:Cynomolgus macaques (3.7-5.7 kg; 5-6 years)[1]
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Dosage:3 mg/kg (Pharmacokinetic Analysis)
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Administration:A single p.o.
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Result:t1/2=4.2 h, Cmax=162 ng/mL, CL/F=41 mL/min/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 936345-35-6
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Appearance Solid
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Peso molecular 359.44
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Fòrmula C18H21N3O3S
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Color White to light yellow
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SMILES
N#CC1=C(C)C=C(OC2=C(C)N(CS(=O)(C)=O)N=C2C3CC3)C=C1C
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Synonyms
PF-2413873
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (278.21 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (3.48 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.48 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Howe DC, et, al. The translational efficacy of a nonsteroidal progesterone receptor antagonist, 4-[3-cyclopropyl-1-(mesylmethyl)-5-methyl-1H-pyrazol-4-yl]oxy,-2,6-dimethylbenzonitrile (PF-02413873), on endometrial growth in macaque and human. J Pharmacol Exp Ther. 2011 Nov;339(2):642-53. [Content Brief]
[2]. Bungay PJ, et, al. Preclinical and clinical pharmacokinetics of PF-02413873, a nonsteroidal progesterone receptor antagonist. Drug Metab Dispos. 2011 Aug;39(8):1396-405. [Content Brief]
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 | 2.7821 mL | 13.9105 mL | 27.8211 mL | 69.5526 mL |
| 5 mM | 0.5564 mL | 2.7821 mL | 5.5642 mL | 13.9105 mL | |
| 10 mM | 0.2782 mL | 1.3911 mL | 2.7821 mL | 6.9553 mL | |
| 15 mM | 0.1855 mL | 0.9274 mL | 1.8547 mL | 4.6368 mL | |
| 20 mM | 0.1391 mL | 0.6955 mL | 1.3911 mL | 3.4776 mL | |
| 25 mM | 0.1113 mL | 0.5564 mL | 1.1128 mL | 2.7821 mL | |
| 30 mM | 0.0927 mL | 0.4637 mL | 0.9274 mL | 2.3184 mL | |
| 40 mM | 0.0696 mL | 0.3478 mL | 0.6955 mL | 1.7388 mL | |
| 50 mM | 0.0556 mL | 0.2782 mL | 0.5564 mL | 1.3911 mL | |
| 60 mM | 0.0464 mL | 0.2318 mL | 0.4637 mL | 1.1592 mL | |
| 80 mM | 0.0348 mL | 0.1739 mL | 0.3478 mL | 0.8694 mL | |
| 100 mM | 0.0278 mL | 0.1391 mL | 0.2782 mL | 0.6955 mL |
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