| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
MW 2474 specifically targets Lysine Acetyltransferase KAT6A (KAT6A). KAT6A is a histone acetyltransferase that acetylates histone H3 at lysine 9 (H3K9) and lysine 23 (H3K23), thereby regulating the transcription of genes involved in cell cycle progression, differentiation, and senescence. By inhibiting the enzymatic activity of KAT6A, MW 2474 prevents the acetylation of these histone marks, leading to the activation of senescence-associated pathways and the suppression of cancer cell proliferation. The compound shows potent inhibition of KAT6A and is a valuable tool for studying the biological functions of this acetyltransferase in both normal and malignant cells.
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| ln Vitro |
In vitro studies have demonstrated that MW 2474 is a potent inhibitor of KAT6A, effectively blocking its histone acetyltransferase activity. As a senescence-inducing agent, MW 2474 has been shown to suppress the proliferation of various cancer cell lines by inducing a senescent phenotype. This activity is attributed to the inhibition of KAT6A-mediated histone acetylation, which results in the transcriptional reprogramming of genes associated with cell cycle arrest and senescence. Its potency and specificity make MW 2474 a valuable chemical probe for in vitro studies aimed at dissecting the molecular pathways governed by KAT6A and its role in tumorigenesis.
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| ln Vivo |
In vivo data for MW 2474 is limited as it is primarily a research tool. However, as a potent KAT6A inhibitor with senescence-inducing properties, it is hypothesized to have significant anti-tumor activity in animal models. In vivo studies with KAT6A inhibitors have shown that targeting this enzyme can lead to tumor growth inhibition by inducing senescence and altering the tumor microenvironment. MW 2474 is available for research use to evaluate its pharmacokinetic properties and anti-cancer efficacy in preclinical models. Further studies are required to fully characterize its in vivo activity, safety, and therapeutic potential.
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| Enzyme Assay |
Non-cellular enzyme/receptor binding assays for MW 2474 typically involve measuring its inhibitory activity against purified recombinant KAT6A enzyme. These assays use a histone substrate (e.g., a peptide derived from histone H3) and radio-labeled or fluorescently-labeled acetyl-CoA as the acetyl donor. The incorporation of acetyl groups into the substrate is measured, and the inhibition by MW 2474 is assessed by determining the half-maximal inhibitory concentration (IC50). These assays are essential for confirming the direct inhibition of KAT6A and for characterizing the compound's potency and selectivity against other acetyltransferases.
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| Cell Assay |
In vitro cell-based assays for MW 2474 are conducted using cancer cell lines to evaluate its cellular effects. Cells are cultured and treated with varying concentrations of MW 2474. The primary readout is often the induction of cellular senescence, which can be measured by assessing senescence-associated beta-galactosidase (SA-β-gal) activity. Other assays include measuring cell proliferation (e.g., via MTT or cell counting), cell cycle analysis by flow cytometry, and the expression of senescence and cell cycle-related markers by Western blotting or qPCR. These experiments help to confirm the on-target activity of MW 2474 and to understand its mechanism of action in a cellular context.
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| Animal Protocol |
In vivo animal studies for MW 2474 are expected to be performed in mouse models of cancer, such as xenograft models. Typically, tumor-bearing mice would be administered MW 2474 via intraperitoneal (i.p.) or oral (p.o.) routes at varying doses. The study would monitor tumor volume, body weight, and overall health to assess efficacy and toxicity. At the end of the study, tumors are harvested for histopathological and biochemical analysis to confirm target modulation (e.g., KAT6A activity, senescence markers) and to evaluate the compound's anti-cancer mechanism. However, specific published in vivo data for MW 2474 are limited.
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| ADME/Pharmacokinetics |
MW 2474 has the molecular formula C18H15FN4O3S and a molecular weight of 386.4 g/mol. It is a small molecule with a LogP of 2.1. The compound is soluble in DMSO. It is recommended to be stored as a powder at -20°C for up to three years or in solution at -80°C for up to one year. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported in publicly available sources. As a research compound, its formulation for in vivo studies often involves DMSO, PEG300, Tween 80, and saline.
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| Toxicity/Toxicokinetics |
Toxicological data for MW 2474 are limited, as it is a research compound not intended for human use. Preliminary in vitro studies in cancer cell lines suggest that it can induce senescence and inhibit proliferation without causing immediate widespread cytotoxicity at certain concentrations. However, comprehensive toxicological profiling, including acute and chronic toxicity studies in animal models, is not publicly available. As with all research compounds, standard safety precautions should be followed when handling MW 2474.
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| Additional Infomation |
MW 2474 is a novel and potent Lysine Acetyltransferase KAT6A inhibitor being developed as a senescence-inducing anti-cancer agent. It has the molecular formula C18H15FN4O3S and CAS number 2414591-05-0. This compound is a valuable tool for studying the role of KAT6A in cancer biology and for evaluating the therapeutic potential of senescence induction. As a research chemical, MW 2474 is not approved for clinical use and is intended for laboratory research purposes only.
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| Molecular Formula |
C18H15FN4O3S
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|---|---|
| Molecular Weight |
386.0849
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| Exact Mass |
386.08
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| Elemental Analysis |
C, 55.95; H, 3.91; F, 4.92; N, 14.50; O, 12.42; S, 8.30
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| CAS # |
2414591-05-0
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| PubChem CID |
154729583
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| Appearance |
Solid powder
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| LogP |
2.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
606
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RKYRWQBKSRLNLX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H15FN4O3S/c1-12-9-14(13-7-8-20-21-11-13)10-16(17(12)19)18(24)22-23-27(25,26)15-5-3-2-4-6-15/h2-11,23H,1H3,(H,22,24)
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| Chemical Name |
N'-(benzenesulfonyl)-2-fluoro-3-methyl-5-pyridazin-4-ylbenzohydrazide
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| Synonyms |
MW-2474; MW 2474; MW2474;
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5901 mL | 12.9507 mL | 25.9014 mL | |
| 5 mM | 0.5180 mL | 2.5901 mL | 5.1803 mL | |
| 10 mM | 0.2590 mL | 1.2951 mL | 2.5901 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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