| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
MAT2A[1]
MAT2A-IN-9 targets MAT2A (methionine adenosyltransferase 2A), an enzyme that catalyzes the synthesis of S-adenosylmethionine (SAM) from methionine and ATP. SAM is a key methyl donor in cellular methylation reactions, and MAT2A is often upregulated in cancers. By inhibiting MAT2A, the compound disrupts methylation metabolism and exhibits antitumor activity. |
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| ln Vitro |
MAT2A-IN-9 demonstrates potent in vitro inhibition of MAT2A. It exhibits antitumor activity against lymphomas and solid tumors. The compound's activity is typically assessed in enzymatic assays measuring MAT2A activity and in cell-based assays evaluating cancer cell proliferation and survival.
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| ln Vivo |
In vivo activity of MAT2A-IN-9 has been suggested by its antitumor activity. The compound has potential for in vivo efficacy in animal models of lymphoma and solid tumors. Further in vivo studies are needed to evaluate its pharmacokinetic properties, antitumor efficacy, and safety profile.
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| Enzyme Assay |
In vitro enzyme assays for MAT2A-IN-9 involve measuring its inhibition of MAT2A activity. The assay typically uses purified recombinant MAT2A enzyme and measures the conversion of methionine and ATP to S-adenosylmethionine (SAM) in the presence of the compound. IC50 values can be determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for MAT2A-IN-9 involve treating cancer cell lines with varying concentrations of the compound and measuring cell proliferation using MTT or other assays. Inhibition of MAT2A activity can be assessed by measuring SAM levels in treated cells using HPLC or mass spectrometry.
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| Animal Protocol |
In vivo animal experiments for MAT2A-IN-9 would typically involve administering the compound to tumor-bearing mouse models of lymphoma or solid tumors. Efficacy is evaluated by measuring tumor growth inhibition, survival rates, and biomarker changes such as SAM levels and methylation markers.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for MAT2A-IN-9 are limited. The compound has a molecular weight of 340.69 and a molecular formula of C14H8ClF3N4O. It is soluble in DMSO at 100 mg/mL (293.52 mM) with ultrasonic treatment. It should be stored at 4°C, away from moisture and light. Its ADME properties have not been fully characterized.
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| Toxicity/Toxicokinetics |
Toxicological data for MAT2A-IN-9 are limited. As a research compound, comprehensive toxicological studies have not been reported. The compound is intended for research use only and is not for human therapeutic application. Standard laboratory safety precautions should be followed when handling this compound.
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| References |
[1]. Muzaffar Alam, et al. 2-oxoquinazoline derivatives as methionine adenosyltransferase 2a inhibitors. WO2020123395A1.
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| Additional Infomation |
MAT2A-IN-9 (CAS#: 2439277-80-0) has the molecular formula C14H8ClF3N4O and a molecular weight of 340.69. It is a 2-oxoquinazoline derivative and a potent MAT2A inhibitor with antitumor activity against lymphomas and solid tumors. It is for research use only.
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| Molecular Formula |
C14H8CLF3N4O
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|---|---|
| Molecular Weight |
340.687731742859
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| Exact Mass |
340.033
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| CAS # |
2439277-80-0
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| PubChem CID |
153608878
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
23
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| Complexity |
513
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
BVNKURJMNQNVAO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H8ClF3N4O/c15-8-3-1-2-4-9(8)22-12-7(11(19)21-13(22)23)5-6-10(20-12)14(16,17)18/h1-6H,(H2,19,21,23)
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| Chemical Name |
4-amino-1-(2-chlorophenyl)-7-(trifluoromethyl)pyrido[2,3-d]pyrimidin-2-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 100 mg/mL (293.52 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9352 mL | 14.6761 mL | 29.3522 mL | |
| 5 mM | 0.5870 mL | 2.9352 mL | 5.8704 mL | |
| 10 mM | 0.2935 mL | 1.4676 mL | 2.9352 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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