2. Epigenetics Metabolic Enzyme/Protease
  3. Methionine Adenosyltransferase (MAT)
  4. AG-270

AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM.

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CAS 番号 : 2201056-66-6

容量 価格（税別） 在庫状況 数量
5 mg $380 在庫あり
10 mg $495 在庫あり
25 mg $800 在庫あり
50 mg $1120 在庫あり
100 mg $1568 在庫あり
500 mg $3200 在庫あり
1 g $4500 在庫あり
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カスタマーレビュー

Based on 10 publication(s) in Google Scholar

AG-270 関連抗体

Top Publications Citing Use of Products

    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.

    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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    • 参考文献

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    製品説明

    AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM[1].
    IC50 & Target

    IC50: 14 nM (MAT2A)[1].
    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    0.257 μM
    Compound: AG-270
    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
    		[PMID: 33829783]
    HCT-116 IC50
    20 μM
    Compound: AG-270
    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
    		[PMID: 33829783]
    HCT-116 IC50
    244 nM
    Compound: AG-270
    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
    		[PMID: 36961373]
    体外実験

    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 関連抗体
    体内実験

    AG-270 shows excellent microsomal, hepatocyte, and in vivo metabolic stability across species (human, mouse, rat, dog, and monkey). AG-270 exhibits T1/2 values of 5.9 h, 4.2 h, 4.8 h and 21.3 h in mouse, rat, monkey and dog, respectively[1].
    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.

    Animal Model: Pancreatic KP4 MTAP-null xenograft mouse model[1].
    Dosage: 10-200 mg/kg.
    Administration: Orally, q.d. for 38 days.
    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).
    臨床実験
    分子量

    489.57

    分子式

    C30H27N5O2
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1C(C2=CC=C(OC)C=C2)=C(NC3=NC=CC=C3)NC4=C(C5=CCCCC5)C(C6=CC=CC=C6)=NN14
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0426 mL 10.2130 mL 20.4261 mL
    5 mM 0.4085 mL 2.0426 mL 4.0852 mL
    10 mM --- --- ---
    View the 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.

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

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    体内:

    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.

    • Protocol 1

      Add each solvent one by one:  15% Cremophor EL    85% Saline

      Solubility: 9.8 mg/mL (20.02 mM); Suspended solution; Need ultrasonic

    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.
    Calculation results:
    Working solution concentration: mg/mL
    純度とドキュメンテーション

    純度: 99.97%

    COA (254 KB) HNMR (281 KB) RP-HPLC (171 KB) LCMS (334 KB)

    取扱説明書 (2659 KB)
    参考文献

    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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    AG-270 Related Classifications

    • Molarity Calculator

    • Dilution Calculator

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    AG-2702201056-66-6AG270AG 270Methionine Adenosyltransferase (MAT)S-adenosylmethionine SynthetaseLowtoxicitypancreaticcancerSAMsolidtumorlymphomaInhibitorinhibitorinhibit

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    製品名:
    AG-270
    製品番号:
    HY-138630
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