PF-06939999
Based on 1 Customer Validation
PF-06939999 (PRMT5-IN-3) is a SAM-competitive, orally active PRMT5 inhibitor that inhibits the expression of SDMA protein (IC50 in A427 is 1.1 nM). PF-06939999 exhibits antitumor effect.
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- Purity: 99.84%
- CAS No.: 2159123-14-3
- 화학식: C22H23F3N4O3
- 분자량:448.44
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
All Histone Methyltransferase Isoforms
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Biological Activity
제품 설명
IC50 & Target
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PRMT5 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
7 nM
Compound: 35
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Antiproliferative activity against human A549 cells
Antiproliferative activity against human A549 cells
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[PMID: 30956011] |
In Vitro
PF-06939999 competitively binds to the cofactor binding site of PRMT5, interferes with its splicing process, leads to splicing changes such as exon skipping and intron retention, thereby affecting cellular functions[2].
PF-06939999 (0.1 nM-10 μM, 7 days) inhibits the proliferation of NSCLC cell A427, NCI-H441, NCI-H1975 and A549, arrests the cell cycle of A427 at G1 phase, arrests the cell cycle of NCI-H1975 at G2/M phase, induces apoptosis in A427 cell[2].
PF-06939999 (30 nM, 10 days) causes cell morphological changes and positive β-galactosidase staining, inducing cell senescence in A549 cell[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A427, NCI-H441, NCI-H1975 and A549
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Concentration:0.1 nM-1 μM
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Incubation Time:5 days
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Result:Inhibited cell proliferation.
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Cell Line:A427 and NCI-H1975
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Concentration:0.3-300 nM
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Incubation Time:5 days
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Result:Arrested the cell cycle of A427 at G1 phase, arrested the cell cycle of NCI-H1975 at G2/M phase.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse A427 or NCI-H441 xenograft models[2]
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Dosage:3-30 mg/kg
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Administration:po, once a day for 36-44 days
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Result:Inhibited tumor growth.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2159123-14-3
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Appearance Solid
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분자량 448.44
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화학식 C22H23F3N4O3
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Color White to off-white
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SMILES
O[C@@H]1[C@H](O)[C@@H](OC2=CC(C(F)F)=C(F)C3=C2CNCC3)C[C@H]1N4C=CC5=C(C)N=CN=C54
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Synonyms
PRMT5-IN-3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
H2O : 100 mg/mL (223.00 mM; Need ultrasonic)
DMSO : ≥ 100 mg/mL (223.00 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.57 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.57 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
순도&문서
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Adli M. Combinatorial drug treatment of cancer. WO2020198601A1.
[2]. Jensen-Pergakes K, et al., SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance. Mol Cancer Ther. 2022 Jan;21(1):3-15. [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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.2300 mL | 11.1498 mL | 22.2995 mL | 55.7488 mL |
| 5 mM | 0.4460 mL | 2.2300 mL | 4.4599 mL | 11.1498 mL | |
| 10 mM | 0.2230 mL | 1.1150 mL | 2.2300 mL | 5.5749 mL | |
| 15 mM | 0.1487 mL | 0.7433 mL | 1.4866 mL | 3.7166 mL | |
| 20 mM | 0.1115 mL | 0.5575 mL | 1.1150 mL | 2.7874 mL | |
| 25 mM | 0.0892 mL | 0.4460 mL | 0.8920 mL | 2.2300 mL | |
| 30 mM | 0.0743 mL | 0.3717 mL | 0.7433 mL | 1.8583 mL | |
| 40 mM | 0.0557 mL | 0.2787 mL | 0.5575 mL | 1.3937 mL | |
| 50 mM | 0.0446 mL | 0.2230 mL | 0.4460 mL | 1.1150 mL | |
| 60 mM | 0.0372 mL | 0.1858 mL | 0.3717 mL | 0.9291 mL | |
| 80 mM | 0.0279 mL | 0.1394 mL | 0.2787 mL | 0.6969 mL | |
| 100 mM | 0.0223 mL | 0.1115 mL | 0.2230 mL | 0.5575 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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