AGI-24512
Based on 2 publication(s) in Google Scholar
AGI-24512 is a potent methionine adenosyltransferase 2α (MAT2A) inhibitor, with an IC50 of 8 nM. AGI-24512 triggers DNA damage response. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro. AGI-24512 can be used for researching anticancer.
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- Purity: 99.46%
- CAS No.: 2201066-53-5
- 화학식: C24H24N4O2
- 분자량:400.47
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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
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Publications Citing Use of MedChemExpress (MCE) AGI-24512
More
Biological Activity
IC50: 8 nM (MAT2A)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.1 μM
Compound: AGI-24512
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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] |
AGI-24512 (0-1 μM; 96 hours) blocks proliferation of MTAP (methylthioadenosine phosphorylase)-deleted HCT116 cancer cells with an IC50 of 100 nM[1].
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AGI-24512 significantly increases in γH2AX-positive cells in MTAP-/- HCT116 cells[1].
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AGI-24512 inhibits PRMT5-mediated SDMA marks with an IC50 of 95 nM in MTAP-/- cells[1].
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AGI-24512 leads to a dose-dependent decrease in SAM (S-adenosylmethionine) levels in the HCT116 MTAP-null cell, with an IC50 of 100 nM[2].
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.
Chemical Information
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CAS No. 2201066-53-5
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Appearance Solid
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분자량 400.47
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화학식 C24H24N4O2
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Color White to gray
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SMILES
O=C1C(C2=CC=C(O)C=C2)=C(C)NC3=C(N4CCCCC4)C(C5=CC=CC=C5)=NN13
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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
Publications (2)
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Journal Impact Factor
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Most Recent
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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 -
Cell Rep
The catalytic efficiency of METTL16 affects cellular processes by governing the intracellular S-adenosylmethionine setpoint. [Abstract]2025 Jul 10;44(7):115966. PMID: 40644296
용액&용해도
DMSO : ≥ 100 mg/mL (249.71 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.
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.
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: ≥ 2.08 mg/mL (5.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (5.19 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (276 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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Kalev P, et al. MAT2A Inhibition Blocks the Growth of MTAP-Deleted Cancer Cells by Reducing PRMT5-Dependent mRNA Splicing and Inducing DNA Damage. Cancer Cell. 2021 Feb 8;39(2):209-224.e11. [Content Brief]
[2]. Konteatis Z, et al. Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion. J Med Chem. 2021 Apr 22;64(8):4430-4449. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4971 mL | 12.4853 mL | 24.9707 mL | 62.4266 mL |
| 5 mM | 0.4994 mL | 2.4971 mL | 4.9941 mL | 12.4853 mL | |
| 10 mM | 0.2497 mL | 1.2485 mL | 2.4971 mL | 6.2427 mL | |
| 15 mM | 0.1665 mL | 0.8324 mL | 1.6647 mL | 4.1618 mL | |
| 20 mM | 0.1249 mL | 0.6243 mL | 1.2485 mL | 3.1213 mL | |
| 25 mM | 0.0999 mL | 0.4994 mL | 0.9988 mL | 2.4971 mL | |
| 30 mM | 0.0832 mL | 0.4162 mL | 0.8324 mL | 2.0809 mL | |
| 40 mM | 0.0624 mL | 0.3121 mL | 0.6243 mL | 1.5607 mL | |
| 50 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 1.2485 mL | |
| 60 mM | 0.0416 mL | 0.2081 mL | 0.4162 mL | 1.0404 mL | |
| 80 mM | 0.0312 mL | 0.1561 mL | 0.3121 mL | 0.7803 mL | |
| 100 mM | 0.0250 mL | 0.1249 mL | 0.2497 mL | 0.6243 mL |
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