AG-270
Based on 14 publication(s) in Google Scholar
AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.97%
- No. CAS: 2201056-66-6
- Fòrmula: C30H27N5O2
- Peso molecular:489.57
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) AG-270
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Nat Commun. 2024 Aug 6;15(1):6672. [Abstract]
- Cell Rep Med. 2025 Jan 20:101925. [Abstract]
- Sci China Life Sci. 2026 May;69(5):1604-1619. [Abstract]
- J Med Chem. 2026 May 14;69(9):10104-10121. [Abstract]
- FASEB J. 2022 Feb;36(2):e22167. [Abstract]
- Anticancer Res. 2026 Feb;46(2):705-712. [Abstract]
- Res Sq. 2026 Jun 15.
- Cancer Diagn Progn. 2026 May 1;6(3):586-595. [Abstract]
- bioRxiv. 2026 May 5.
- Res Sq. 2026 Mar 5.
- University of Wisconsin. 2026.
- MicroPubl Biol. 2025 Sep 4:2025. [Abstract]
- bioRxiv. 2025 July 11.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Flow Cytometry
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Histological Imaging/Staining
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In Vivo Efficacy Study
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WB
Actividad biológica
IC50: 14 nM (MAT2A)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.257 μM
Compound: AG-270
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Antiproliferative activity against MATP-null human HCT-116 cells isogenic cell model assessed as maximal cell growth inhibition at 20 uM incubated for 96 hrs by Cell Titer-Glo assay
Antiproliferative activity against MATP-null human HCT-116 cells isogenic cell model assessed as maximal cell growth inhibition at 20 uM incubated for 96 hrs by Cell Titer-Glo assay
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[PMID: 33829783] |
| HCT-116 | IC50 |
20 μM
Compound: AG-270
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Inhibition of SAM production in human HCT-116 cells isogenic cell model measured after 72 hrs by LC-MS/MS analysis
Inhibition of SAM production in human HCT-116 cells isogenic cell model measured after 72 hrs by LC-MS/MS analysis
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[PMID: 33829783] |
| HCT-116 | IC50 |
244 nM
Compound: AG-270
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Antiproliferative activity against human HCT-116 cells expressing MTAP-/- assessed as inhibition of cell proliferation incubated for 4 days by fluorescence based assay
Antiproliferative activity against human HCT-116 cells expressing MTAP-/- assessed as inhibition of cell proliferation incubated for 4 days by fluorescence based assay
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[PMID: 36961373] |
AG-270 demonstrates potent reduction in levels of intracellular SAM, as well as MTAP-null–selective antiproliferative activity in the HCT116 MTAP isogenic cell model in vitro[1].
AG-270 exhibits an IC50 of 20 nM in HCT116 MTAP-null cell SAM at 72 h[1].
MAT2A is a key enzyme in the methionine salvage pathway, responsible for generating the universal methyl donor, S-adenosylmethionine (SAM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AG-270 (200 mg/kg, orally, q.d. for 38 days) results in dose-dependent reduction in tumor SAM levels and tumor growth of KP4 MTAP-null xenografts and is well tolerated, with mean body weight loss <5%[1].
Combining AG-270 with taxanes and gemcitabine yielded additive-tosynergistic antitumor activity, with the docetaxel combination yielding 50% complete tumor regressions in select models; combination benefits are observed in PDX models derived from esophageal, NSCLC, and pancreatic cancers[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pancreatic KP4 MTAP-null xenograft mouse model[1].
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Dosage:10-200 mg/kg.
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Administration:Orally, q.d. for 38 days.
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Result:Led to dose-dependent reductions in tumor SAM levels and tumor growth of KP4 MTAP-null xenografts (TGI = 36% (10 mg/kg), 48% (30 mg/kg), 66% (100 mg/kg), 67% (200 mg/kg).
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2201056-66-6
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Appearance Solid
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Peso molecular 489.57
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Fòrmula C30H27N5O2
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Color White to off-white
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SMILES
O=C1C(C2=CC=C(OC)C=C2)=C(NC3=NC=CC=C3)NC4=C(C5=CCCCC5)C(C6=CC=CC=C6)=NN14
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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 1 year -20°C 6 months
Publications (14)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
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
AG-270 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Aug 6;15(1):6672. [Abstract]
AG-270 group showed a reduction of Ki-67 compared to the control group and significantly decreased ERG and EZH2 protein levels.
AG-270 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Aug 6;15(1):6672. [Abstract]
Ex-vivo SFA from dissociated LuCaP 35 under treatment with the indicated concentration of AG-270 (0.2, 0.5, 1 μM).
AG-270 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2024 Aug 6;15(1):6672. [Abstract]
Immunoblot with indicated antibodies in LNCaPabl cells after treatment with the indicated dose of AG-270 (0.5 μM).
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Cell Rep Med
Single-cell analysis of neoplastic plasma cells identifies myeloma pathobiology mediators and potential targets. [Abstract]2025 Jan 20:101925. PMID: 39855192
AG-270 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2025 Jan 20:101925. [Abstract]
Effect of AG-270 over 24–72 h on viability in these cell lines evaluated with WST-1.
AG-270 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2025 Jan 20:101925. [Abstract]
Cell cycle distribution in ANBL-6 cells treated with AG-270 (1, 2, 4 μM, 6-72 h) and analyzed by flow after PI staining.
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Sci China Life Sci
2026 May;69(5):1604-1619. PMID: 41793590 -
J Med Chem
Design and Discovery of Pyridazinone-Based MAT2A Inhibitors Targeting MTAP-Deficient Cancers. [Abstract]2026 May 14;69(9):10104-10121. PMID: 42024642 -
FASEB J
Inhibition of MAT2A suppresses osteoclastogenesis and prevents ovariectomy-induced bone loss. [Abstract]2022 Feb;36(2):e22167. PMID: 35064691 -
Anticancer Res
Lack of Cancer Specificity of Methionine Adenosyltransferase 2A (MAT2A) Inhibitor AG-270 in Combination With Recombinant Methioninase In Vitro. [Abstract]2026 Feb;46(2):705-712. PMID: 41617456 -
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Cancer Diagn Progn
The Combination of Methionine Adenosyltransferase 2A (MAT2A) Inhibitor AG-270 and Recombinant Methioninase Is Not Cancer-selective in a Co-culture Model of Colon Cancer Cells and Normal Fibroblasts. [Abstract]2026 May 1;6(3):586-595. PMID: 42078306 -
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MicroPubl Biol
CD320 expression is increased in breast cancer stem cells but does not promote their expansion or alter key histone methylation marks. [Abstract]2025 Sep 4:2025. PMID: 40985010 -
Solvente y solubilidad
DMSO : 4 mg/mL (8.17 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 15% Cremophor EL 85% Saline
Solubility: 9.8 mg/mL (20.02 mM); Suspended solution; Need ultrasonic
Pureza y Documentación
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Ficha de datos (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0426 mL | 10.2130 mL | 20.4261 mL | 51.0652 mL |
| 5 mM | 0.4085 mL | 2.0426 mL | 4.0852 mL | 10.2130 mL |
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