PF-06726304
Based on 1 publication(s) in Google Scholar
PF-06726304 is a potent and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 displays robust antitumor growth activity.
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- Purity: 99.71%
- CAS No.: 1616287-82-1
- 화학식: C22H21Cl2N3O3
- 분자량:446.33
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
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Epigenetics Compound Library
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Publications Citing Use of MedChemExpress (MCE) PF-06726304
MoreAll Histone Methyltransferase Isoforms
More
Biological Activity
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EZH2 WT 0.7 nM (Ki) |
EZH2 Y641N 3.0 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KARPAS-422 | IC50 |
122 nM
Compound: 2; PF-06726304
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Antiproliferative activity against human KARPAS-422 cells assessed as cell growth inhibition incubated for 72 hrs followed by compound dilution in growth medium and measured after 96 hrs by Alamar blue assay
Antiproliferative activity against human KARPAS-422 cells assessed as cell growth inhibition incubated for 72 hrs followed by compound dilution in growth medium and measured after 96 hrs by Alamar blue assay
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[PMID: 35300079] |
| KARPAS-422 | IC50 |
23 nM
Compound: 1
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Antiproliferative activity against human KARPAS422 cells after 72 hrs by resazurin assay
Antiproliferative activity against human KARPAS422 cells after 72 hrs by resazurin assay
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[PMID: 29211475] |
| KARPAS-422 | IC50 |
23 nM
Compound: 1
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Inhibition of cell proliferation in human KARPAS-422 cells
Inhibition of cell proliferation in human KARPAS-422 cells
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[PMID: 33529029] |
| KARPAS-422 | IC50 |
25 nM
Compound: 31
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Cytotoxicity against human KARPAS422 cells assessed as inhibition of cell proliferation after 72 hrs
Cytotoxicity against human KARPAS422 cells assessed as inhibition of cell proliferation after 72 hrs
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[PMID: 27512831] |
PF-06726304 (Compound 31) inhibits H3K27me3 in Karpas-422 with an IC50 of 15 nM[1].
PF-06726304 inhibits the proliferation of Karpas-422 cells that harbor wild-type EZH2 with an IC50 of 25 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Scid beige mice (6-8 weeks old) with Karpas-422 xenograft model[1]
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Dosage:200 and 300 mg/kg
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Administration:Given BID for 20 days
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Result:Inhibited tumor growth and induced robust modulation of downstream biomarkers in a subcutaneous Karpas-422 xenograft model.
Chemical Information
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CAS No. 1616287-82-1
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Appearance Solid
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분자량 446.33
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화학식 C22H21Cl2N3O3
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Color White to off-white
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SMILES
O=C1N(CC2=C(C)C=C(C)NC2=O)CCC3=C1C(Cl)=C(C4=C(C)ON=C4C)C=C3Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Front Cell Dev Biol
EZH2/EHMT2 Histone Methyltransferases Inhibit the Transcription of DLX5 and Promote the Transformation of Myelodysplastic Syndrome to Acute Myeloid Leukemia. [Abstract]2021 Aug 2;9:619795. PMID: 34409024
용액&용해도
DMSO : ≥ 15 mg/mL (33.61 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, 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.
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.
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 mg/mL (2.24 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (2.24 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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.
순도&문서
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Data Sheet (275 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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Handling Instructions (2659 KB)
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 | 2.2405 mL | 11.2025 mL | 22.4049 mL | 56.0124 mL |
| 5 mM | 0.4481 mL | 2.2405 mL | 4.4810 mL | 11.2025 mL | |
| 10 mM | 0.2240 mL | 1.1202 mL | 2.2405 mL | 5.6012 mL | |
| 15 mM | 0.1494 mL | 0.7468 mL | 1.4937 mL | 3.7342 mL | |
| 20 mM | 0.1120 mL | 0.5601 mL | 1.1202 mL | 2.8006 mL | |
| 25 mM | 0.0896 mL | 0.4481 mL | 0.8962 mL | 2.2405 mL | |
| 30 mM | 0.0747 mL | 0.3734 mL | 0.7468 mL | 1.8671 mL |
PF-06726304 Related Classifications
HY-103682 Related Classifications
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