| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
| Targets |
MAT2A[1]
MAT2A inhibitor 4 targets the catalytic subunit of methionine S-adenosyltransferase-2 (MAT2A). MAT2A is an enzyme that catalyzes the production of S-adenosylmethionine (SAM) from methionine and ATP. SAM is a major methyl donor for DNA and histone methylation. By inhibiting MAT2A, this compound disrupts methionine metabolism and epigenetic regulation. |
|---|---|
| ln Vitro |
Methionine S-adenosyltransferase-2's catalytic subunit is inhibited by MAT2A inhibitor 4[1].
In vitro, MAT2A inhibitor 4 demonstrates potent inhibition of MAT2A enzymatic activity. It exhibits potent antitumor activity, selectively targeting MTAP-deficient tumor cells while sparing normal tissues. This selectivity makes it a valuable tool for studying methionine metabolism and epigenetic vulnerabilities in cancer. |
| ln Vivo |
In vivo data for MAT2A inhibitor 4 is not extensively reported in publicly available sources. As a potent MAT2A inhibitor with selective antitumor activity, the compound has potential applications in animal models of cancer, particularly MTAP-deficient tumors. However, specific published in vivo efficacy studies are not detailed in the current literature. MAT2A inhibitor 4 is primarily used as a research tool for studying methionine metabolism and cancer.
|
| Enzyme Assay |
The in vitro MAT2A inhibition assay for MAT2A inhibitor 4 uses recombinant MAT2A enzyme and substrates methionine and ATP. Enzyme activity is measured by quantifying the production of S-adenosylmethionine (SAM) using HPLC or mass spectrometry. The compound is added at various concentrations, and IC50 values are calculated from dose-response curves. Selectivity for MAT2A over MAT1A is confirmed by profiling against the related enzyme.
|
| Cell Assay |
Cellular assays for MAT2A inhibitor 4 are conducted in cancer cell lines, particularly those that are MTAP-deficient. Cells are treated with varying concentrations of the compound. Cell viability and proliferation are measured using standard assays such as MTT or CellTiter-Glo. SAM levels and DNA/histone methylation are measured to assess the compound's effects on methionine metabolism and epigenetics.
|
| Animal Protocol |
In vivo studies for MAT2A inhibitor 4 would typically involve xenograft mouse models of MTAP-deficient tumors. The compound would be administered via oral or intraperitoneal routes. Efficacy would be assessed by measuring tumor growth inhibition. Pharmacodynamic markers such as SAM levels and methylation status would be evaluated in tumor tissues. However, specific published in vivo protocols for MAT2A inhibitor 4 are not available.
|
| ADME/Pharmacokinetics |
MAT2A inhibitor 4 has a molecular formula of C16H15ClFN and a molecular weight of 275.75. It has a CAS number of 1391934-91-0. As a small molecule, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life and bioavailability are not extensively reported in the provided sources.
|
| Toxicity/Toxicokinetics |
Toxicity data for MAT2A inhibitor 4 is limited. As with all research compounds, MAT2A inhibitor 4 is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
|
| References | |
| Additional Infomation |
MAT2A inhibitor 4 (CAS 1391934-91-0) is an inhibitor of the catalytic subunit of methionine S-adenosyltransferase-2 (MAT2A). It exhibits potent antitumor activity, selectively targeting MTAP-deficient tumor cells. It is used in cancer research. It has a molecular formula of C16H15ClFN and a molecular weight of 275.75. It is for research use only.
|
| Molecular Formula |
C16H15CLFN
|
|---|---|
| Molecular Weight |
275.748406648636
|
| Exact Mass |
275.087
|
| CAS # |
1391934-91-0
|
| PubChem CID |
60141313
|
| Appearance |
Light yellow to green yellow solid powder
|
| LogP |
5
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
19
|
| Complexity |
297
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
ClC1C=CC=C(C=1/C=C/C1C=CC(=CC=1)N(C)C)F
|
| InChi Key |
ZAXUUHSGXRGGON-DHZHZOJOSA-N
|
| InChi Code |
InChI=1S/C16H15ClFN/c1-19(2)13-9-6-12(7-10-13)8-11-14-15(17)4-3-5-16(14)18/h3-11H,1-2H3/b11-8+
|
| Chemical Name |
4-[(E)-2-(2-chloro-6-fluorophenyl)ethenyl]-N,N-dimethylaniline
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : 250 mg/mL (906.62 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.54 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6265 mL | 18.1324 mL | 36.2647 mL | |
| 5 mM | 0.7253 mL | 3.6265 mL | 7.2529 mL | |
| 10 mM | 0.3626 mL | 1.8132 mL | 3.6265 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
