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| Targets |
M2N12 targets cell division cycle 25 (Cdc25) phosphatases, specifically Cdc25C. Cdc25 phosphatases are key regulators of the cell cycle, activating cyclin-dependent kinases (CDKs) by dephosphorylating them. Cdc25C specifically activates CDK1, which is essential for entry into mitosis. By inhibiting Cdc25C with high potency (IC50 = 0.09 μM), M2N12 blocks cell cycle progression.
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| ln Vitro |
M2N12 (0-20 μM; 72 hours) exhibits cytotoxic activity against A-549, MDA-MB-231, KB, KB-VIN, MCF-7, and HBE tumor cell lines as well as a normal cell line (IC50=3.92 μM, 4.63 μM, 5.05 μM, 6.81 μM, 4.71 μM, and 6.00 μM, respectively)[1].
In vitro, M2N12 potently inhibits Cdc25C with an IC50 of 0.09 μM. It also shows activity against Cdc25A (IC50 = 0.53 μM) and Cdc25B (IC50 = 1.39 μM). As a potent and highly selective Cdc25C inhibitor, M2N12 has antitumor activity. These in vitro activities support its use in studying cell cycle regulation and cancer. |
| ln Vivo |
In vivo data for M2N12 is not extensively reported in publicly available sources. As a potent Cdc25C inhibitor with antitumor activity, the compound has potential applications in animal models of cancer. However, specific published in vivo efficacy studies are not detailed in the current literature. M2N12 is primarily used as a research tool for studying cell cycle regulation and cancer biology.
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| Enzyme Assay |
The in vitro Cdc25 phosphatase inhibition assay for M2N12 uses recombinant Cdc25A, Cdc25B, and Cdc25C enzymes and a fluorogenic substrate. Enzyme activity is measured by quantifying the dephosphorylation of the substrate. The compound is added at various concentrations, and IC50 values are calculated from dose-response curves. Selectivity profiling against other phosphatases is performed to confirm specificity.
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| Cell Assay |
Cellular assays for M2N12 are conducted in cancer cell lines. Cells are treated with varying concentrations of M2N12. Cell cycle analysis is performed by flow cytometry to assess the compound's effects on cell cycle progression. Cell viability and proliferation are measured using standard assays such as MTT or CellTiter-Glo. The phosphorylation status of CDK1 and other cell cycle regulators is assessed by Western blotting.
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| Animal Protocol |
In vivo studies for M2N12 would typically involve xenograft mouse models of cancer. The compound would be administered via oral or intraperitoneal routes. Efficacy would be assessed by measuring tumor growth inhibition. Pharmacodynamic markers such as cell cycle progression and CDK1 phosphorylation would be evaluated in tumor tissues. However, specific published in vivo protocols for M2N12 are not available in the current literature.
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| ADME/Pharmacokinetics |
M2N12 has a molecular weight of 393.83 and a molecular formula of C20H16ClN5O2. It has a CAS number of 2376577-06-7. 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.
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| Toxicity/Toxicokinetics |
Toxicity data for M2N12 is limited. As with all research compounds, M2N12 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.
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| References | |
| Additional Infomation |
M2N12 (CAS 2376577-06-7) is a potent and highly selective inhibitor of Cdc25C (IC50 = 0.09 μM). It also inhibits Cdc25A (IC50 = 0.53 μM) and Cdc25B (IC50 = 1.39 μM). M2N12 has antitumor activity and is used in cancer research. It has a molecular formula of C20H16ClN5O2 and a molecular weight of 393.83. It is for research use only.
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| Molecular Formula |
C20H16CLN5O2
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|---|---|
| Molecular Weight |
393.8263
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| Exact Mass |
393.099
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| CAS # |
2376577-06-7
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| Related CAS # |
M5N36;2832887-40-6
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| PubChem CID |
139600304
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| Appearance |
Brown to red solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
647
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C(C2C([H])=C([H])C([H])=NC=2C(C=1N([H])C([H])([H])C1=C([H])N(C([H])([H])C2C([H])=C([H])C(C([H])([H])[H])=C([H])C=2[H])N=N1)=O)=O
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| InChi Key |
BDBIMDYALUJAPR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H16ClN5O2/c1-12-4-6-13(7-5-12)10-26-11-14(24-25-26)9-23-18-16(21)19(27)15-3-2-8-22-17(15)20(18)28/h2-8,11,23H,9-10H2,1H3
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| Chemical Name |
6-chloro-7-[[1-[(4-methylphenyl)methyl]triazol-4-yl]methylamino]quinoline-5,8-dione
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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 |
| 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 : 11.11 mg/mL (28.21 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.11 mg/mL (2.82 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 11.1 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5392 mL | 12.6958 mL | 25.3917 mL | |
| 5 mM | 0.5078 mL | 2.5392 mL | 5.0783 mL | |
| 10 mM | 0.2539 mL | 1.2696 mL | 2.5392 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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