| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
The primary target of MOMA-341 is the Werner RecQ‑like helicase (WRN). WRN is a helicase involved in DNA replication, repair, recombination, and transcription. MOMA-341 binds to WRN at cysteine 727 through an allosteric and ATP‑competitive binding mechanism. Inhibition of WRN induces DNA damage and is synthetic lethal in cancer cells that are deficient in DNA mismatch repair (dMMR) or have high levels of microsatellite instability (MSI-H).
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| ln Vitro |
In vitro, MOMA-341 binds to WRN at cysteine 727 via an allosteric and ATP-competitive binding mechanism. It induces DNA damage and tumor regression in dMMR/MSI‑H models. It shows anti‑tumor activity, which is currently being evaluated in advanced and metastatic solid tumors research. The exact IC₅0 for WRN inhibition has not been published in the provided material.
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| ln Vivo |
MOMA-341 can induce DNA damage, cell death and tumor elimination in a mismatch repair deficient (dMMR)/microsatellite instability high (MSI-H) model [1].
In vivo, MOMA-341 has antitumor activity and can be used for advanced and metastatic solid tumors research. In mouse xenograft models of dMMR/MSI‑H solid tumors, MOMA-341 induces tumor regression. Its mechanism of inducing DNA damage leads to cell death specifically in cancer cells that rely on WRN for survival. |
| Enzyme Assay |
Non-cell-based (cell-free) experiments for MOMA-341 focus on direct enzyme inhibition. A standard protocol uses recombinant WRN helicase protein. The enzyme is incubated with a fluorescently labeled DNA substrate (e.g., a fork or G‑quadruplex structure) in a reaction buffer containing ATP. Increasing concentrations of MOMA-341 (0.1 nM to 10 uM) are added, and the reaction proceeds for 30-60 min at 37degC. The unwinding of the DNA substrate leads to a change in fluorescence polarization or FRET signal. The IC₅0 for inhibition of WRN helicase activity is calculated from the dose-response curve. The binding mode (ATP‑competitive, allosteric) is confirmed by measuring the IC₅0 in the presence of varying ATP concentrations (Lineweaver‑Burk analysis) or by performing a drug affinity responsive target stability (DARTS) assay.
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| Cell Assay |
Cell-based assays for MOMA-341 are conducted in dMMR/MSI‑H cancer cell lines (e.g., HCT116, LoVo). Cells are seeded in 96‑well plates and treated with increasing concentrations of MOMA-341 (0.001-10 uM) for 72-96 hours. Cell viability is measured by CellTiter‑Glo or MTT assay. The IC₅0 for growth inhibition is calculated. DNA damage is assessed by Western blotting or immunofluorescence for gammaH2AX (a marker of double‑strand breaks). The cell cycle can be analyzed by flow cytometry after propidium iodide staining to detect an S‑phase or G2/M arrest. Apoptosis is measured by Annexin V/PI staining.
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| Animal Protocol |
In vivo animal experiments for MOMA-341 are conducted in mouse xenograft models of dMMR/MSI‑H solid tumors. Nude mice are implanted subcutaneously with HCT116 or LoVo cells. Once tumors reach a certain size (e.g., 100-200 mm3), mice are randomized to treatment groups. MOMA-341 is administered orally or intraperitoneally at doses ranging from 1 to 100 mg/kg daily or every other day for 2-4 weeks. Tumor volume is measured by calipers twice weekly. Plasma and tumor tissue are collected at endpoint to measure compound concentration and target engagement. The effect on DNA damage in tumor tissue is assessed by immunohistochemistry (IHC) for gammaH2AX.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for MOMA-341 are limited. The compound has a molecular weight of 570.54 g/mol and a molecular formula of C2₈H2₆F4N₆O3. It appears as a solid at room temperature (melting point not reported). The compound is typically stored at -20degC, protected from light. It is soluble in DMSO and organic solvents.
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| Toxicity/Toxicokinetics |
The toxicity of MOMA-341 is not fully characterized. As a research chemical that targets DNA repair mechanisms, it may be toxic to rapidly dividing cells. Standard safety precautions apply: the compound may be harmful if swallowed, inhaled, or absorbed through the skin. It may cause skin and eye irritation. It should be handled in a well-ventilated area (fume hood) with appropriate PPE (lab coat, gloves, safety goggles). The product is not for human use.
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| References | |
| Additional Infomation |
Additional information: The compound has a CAS number of 3078276-74-8. It is also known as an ATP‑competitive WRN allosteric inhibitor (Cys727 site). The compound is for research use only and is not for human or veterinary use.
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| Molecular Formula |
C28H26F4N6O3
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|---|---|
| Molecular Weight |
570.54
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| Exact Mass |
570.2
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| CAS # |
3078276-74-8
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| PubChem CID |
176317256
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| Appearance |
Typically exists as solids at room temperature
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| Hydrogen Bond Donor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
41
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| Complexity |
1030
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C=CC(=O)N1CCC2=NN(C3=C2[C@H](C1)N(CC3)C(=O)C4=CN=C(C(=C4N)F)C(F)(F)F)C5=C(C=C(C=C5)C6CC6)O
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| InChi Key |
XGLVNFVYNNRPRE-FQEVSTJZSA-N
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| InChi Code |
InChI=1S/C28H26F4N6O3/c1-2-22(40)36-9-7-17-23-19(38(35-17)18-6-5-15(11-21(18)39)14-3-4-14)8-10-37(20(23)13-36)27(41)16-12-34-26(28(30,31)32)24(29)25(16)33/h2,5-6,11-12,14,20,39H,1,3-4,7-10,13H2,(H2,33,34)/t20-/m0/s1
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| Chemical Name |
1-[(8R)-7-[4-amino-5-fluoro-6-(trifluoromethyl)pyridine-3-carbonyl]-3-(4-cyclopropyl-2-hydroxyphenyl)-2,3,7,10-tetrazatricyclo[6.4.1.04,13]trideca-1,4(13)-dien-10-yl]prop-2-en-1-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 |
| 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 | 1.7527 mL | 8.7636 mL | 17.5273 mL | |
| 5 mM | 0.3505 mL | 1.7527 mL | 3.5055 mL | |
| 10 mM | 0.1753 mL | 0.8764 mL | 1.7527 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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