PF-9366
Based on 18 publication(s) in Google Scholar
PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor, with an IC50 of 420 nM and a Kd of 170 nM.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.94%
- CAS No.: 72882-78-1
- 화학식: C20H19ClN4
- 분자량:350.84
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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
- Protocol
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) PF-9366
More- Cell. 2020 Jun 11;181(6):1329-1345.e24. [Abstract]
- Nat Cancer. 2022 May;3(5):629-648. [Abstract]
- Immunity. 2021 Aug 10;54(8):1728-1744.e7. [Abstract]
- Cancer Commun (Lond). 2025 Nov 10. [Abstract]
- Nat Metab. 2023 Nov;5(11):1911-1930. [Abstract]
- Mol Cell. 2021 May 20;81(10):2076-2093.e9. [Abstract]
- Mol Cell. 2019 Sep 19;75(6):1147-1160.e5. [Abstract]
- Nat Commun. 2025 Jul 1;16(1):6016. [Abstract]
- Nat Commun. 2024 Aug 6;15(1):6672. [Abstract]
- Sci China Life Sci. 2026 May;69(5):1604-1619. [Abstract]
- EMBO J. 2022 Sep 1;41(17):e111608. [Abstract]
- Cancer Immunol Res. 2024 Aug 1;12(8):1039-1057. [Abstract]
- J Orthop Translat. 2025 Oct 16:55:346-359. [Abstract]
- PLoS Biol. 2022 Feb 10;20(2):e3001535. [Abstract]
- Front Cell Dev Biol. 2021 Mar 30:9:633259. [Abstract]
- J Biol Chem. 2022 Sep;298(9):102367. [Abstract]
- Cell J. 2022 Apr;24(4):204-211. [Abstract]
- SSRN. 2024 Jul 02.
Customer Validation & Images
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WB
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IF
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RT-PCR
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
Biological Activity
PF-9366 is a Mat2A inhibitor, with an IC50 of 420 nM and a Kd of 170 nM. PF-9366 displays no substantial off-target activity in GPCRs, neurotransporters, phosphodiesterases, and ion channels. PF-9366 has inhibitory activity against Mat2A in cancer cells. PF-9366 inhibits cellular S-Adenosyl-L-methionine (SAM) production with an IC50 of 1.2 μM in H520 lung carcinoma cells. PF-9366 is more potent in Huh-7 cells against SAM synthesis, with an IC50 of 255 nM, and also suppresses the proliferation of cells with an IC50 of 10 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 72882-78-1
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Appearance Solid
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분자량 350.84
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화학식 C20H19ClN4
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Color White to off-white
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SMILES
CN(C)CCC1=NN=C2N1C3=CC=C(Cl)C=C3C(C4=CC=CC=C4)=C2
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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 (18)
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Journal Impact Factor
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Most Recent
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Cell
2020 Jun 11;181(6):1329-1345.e24. PMID: 32445698 -
Nat Cancer
Loss of MAT2A compromises methionine metabolism and represents a vulnerability in H3K27M mutant glioma by modulating the epigenome. [Abstract]2022 May;3(5):629-648. PMID: 35422502 -
Immunity
Multiomics analyses reveal a critical role of selenium in controlling T cell differentiation in Crohn's disease. [Abstract]2021 Aug 10;54(8):1728-1744.e7. PMID: 34343498 -
Cancer Commun (Lond)
Unfolded protein response kinase PERK supports survival and metastasis of circulating tumor cell clusters via SAM synthesis and H3K4me3-dependent PDGFB signaling. [Abstract]2025 Nov 10. PMID: 41212905 -
Nat Metab
2023 Nov;5(11):1911-1930. PMID: 37973897 -
Mol Cell
mTORC1 stimulates cell growth through SAM synthesis and m6A mRNA-dependent control of protein synthesis. [Abstract]2021 May 20;81(10):2076-2093.e9. PMID: 33756106
PF-9366 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2021 May 20;81(10):2076-2093.e9. [Abstract]
Relative incorporation of the radiolabel from (C3H3)-methionine into total RNA from wild-type HeLa cells grown in the absence of serum and treated with vehicle, insulin (500 nM), rapamycin (20 nM) or MAT2A inhibitor (PF-9366, 10 μM) for 24 hours.
PF-9366 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2021 May 20;81(10):2076-2093.e9. [Abstract]
Cancer cell lines treated with vehicle or MAT2Ai (PF-9366, 10 μM) were grown in 1% serum for 72 hours, and Cell Titer-Glo measurements were performed every 24 hours.
PF-9366 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2021 May 20;81(10):2076-2093.e9. [Abstract]
PDX of breast cancer bearing TP53 and PIK3CAH1047 mutations was subcutaneously injected into the flanks of NOD.Cg-Prkdcscid Il2rgtm1Wj1/SzJ mice. Mice were randomized 1:1 to receive vehicle (PEG/Tween 5%) or MAT2Ai (PF-9366, 50 mg/kg), and tumor volume was monitored over time.
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Mol Cell
One-Carbon Metabolism Supports S-Adenosylmethionine and Histone Methylation to Drive Inflammatory Macrophages. [Abstract]2019 Sep 19;75(6):1147-1160.e5. PMID: 31420217 -
Nat Commun
2025 Jul 1;16(1):6016. PMID: 40593722 -
Nat Commun
Epigenome-wide impact of MAT2A sustains the androgen-indifferent state and confers synthetic vulnerability in ERG fusion-positive prostate cancer. [Abstract]2024 Aug 6;15(1):6672. PMID: 39107274 -
Sci China Life Sci
2026 May;69(5):1604-1619. PMID: 41793590 -
EMBO J
Attenuation of SARS-CoV-2 replication and associated inflammation by concomitant targeting of viral and host cap 2'-O-ribose methyltransferases. [Abstract]2022 Sep 1;41(17):e111608. PMID: 35833542 -
Cancer Immunol Res
mTOR signaling promotes rapid m6A mRNA methylation to regulate NK-cell activation and effector functions. [Abstract]2024 Aug 1;12(8):1039-1057. PMID: 38640466 -
J Orthop Translat
Targeting MAT2A synergistically induces DNA damage in osteosarcoma cells through EZH2-mediated H3K27me3 modification. [Abstract]2025 Oct 16:55:346-359. PMID: 41146859
PF-9366 purchased from MedChemExpress. Usage Cited in: J Orthop Translat. 2025 Oct 16:55:346-359. [Abstract]
Western blot analysis of MAT2A protein levels in 143B cells treated with PF-9366 at different concentrations (0.5 μM, 1 μM, 2 μM, 4 μM, 6 μM) for 72 h.
PF-9366 purchased from MedChemExpress. Usage Cited in: J Orthop Translat. 2025 Oct 16:55:346-359. [Abstract]
Immunofluorescence staining of DAPI and γH2AX in osteosarcoma cells treated with GSK126 and PF-9366.
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PLoS Biol
Dynamic assembly of the mRNA m6A methyltransferase complex is regulated by METTL3 phase separation. [Abstract]2022 Feb 10;20(2):e3001535. PMID: 35143475 -
Front Cell Dev Biol
2021 Mar 30:9:633259. PMID: 33859984 -
J Biol Chem
Extracellular 5'-methylthioadenosine inhibits intracellular symmetric dimethylarginine protein methylation of FUSE-binding proteins. [Abstract]2022 Sep;298(9):102367. PMID: 35963436 -
Cell J
Inhibition of MAT2A-Related Methionine Metabolism Enhances The Efficacy of Cisplatin on Cisplatin-Resistant Cells in Lung Cancer. [Abstract]2022 Apr;24(4):204-211. PMID: 35674024 -
용액&용해도
DMSO : 10 mg/mL (28.50 mM; Need ultrasonic; 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, 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: ≥ 2.5 mg/mL (7.13 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.
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.
Protocol
The Mat2A and Mat2B proteins are extensively dialyzed into a buffer containing 150 mM KCl, 25 mM HEPES, pH 7.4, 5 mM MgCl2, 5% (v/v) glycerol, 2 mM TCEP. Concentrations are determined spectrophotometrically using an ɛ280 of 44,350 /M.cm for Mat2A and an ɛ280 of 36,440 /M.cm for Mat2B. Compounds (PF-9366) are diluted from 100% DMSO stocks into a buffer without DMSO. In a typical experiment, nineteen 15 μL injections of 200 μM compound or 30-35 μM Mat2B are made into 10 μM Mat2A on a VP ITC or nineteen 2 μL injections of 200 μM compound into 10 μM Mat2A on an Auto iTC200. Data are analyzed and fit to a simple 1:1 binding model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Huh-7 cells are seeded at a concentration of 15,000 cells per well for 6-h incubation with compound (PF-9366) and 4,000 cells per well for 72-h incubation with compound in 96-well plates in 200 μL of growth medium. NCI-H520 MAT2B knockdown cells are seeded at a concentration of 20,000 cells per well for 6 h incubation or 10,000 cells per well for 72 h incubation with compound in 96 well plates in 200 μL of growth medium. Cells are allowed to attach overnight at 37°C with 5% CO2. A 5× solution of cycloleucine is prepared fresh from powder stock in growth medium. Other compounds (PF-9366) are diluted in 100% DMSO using a three-fold dilution scheme and further diluted in growth medium to give 0.5% DMSO final. Consistency of cellular confluence for each cell line is monitored with the IncuCyte Zoom live cell imager. Proliferation is measured using CellTiterGlo reagent. Growth media is removed from the cell plates following compound treatment and 80 μL/well CellTiter Glo diluted 1:1 in PBS added. Luminescence is measured by an Plate Reader[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (279 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 | 2.8503 mL | 14.2515 mL | 28.5030 mL | 71.2576 mL |
| 5 mM | 0.5701 mL | 2.8503 mL | 5.7006 mL | 14.2515 mL | |
| 10 mM | 0.2850 mL | 1.4252 mL | 2.8503 mL | 7.1258 mL | |
| 15 mM | 0.1900 mL | 0.9501 mL | 1.9002 mL | 4.7505 mL | |
| 20 mM | 0.1425 mL | 0.7126 mL | 1.4252 mL | 3.5629 mL | |
| 25 mM | 0.1140 mL | 0.5701 mL | 1.1401 mL | 2.8503 mL |
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