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| Targets |
ME-344 targets mitochondrial oxidative phosphorylation (OXPHOS) complex I, a key enzyme in the electron transport chain responsible for ATP generation and oxygen consumption. By inhibiting complex I, ME-344 disrupts mitochondrial respiration and energy production in cancer cells. The compound also inhibits mTOR through downregulation of the AKT/mTOR pathway, contributing to its anticancer activity. This dual mechanism of action makes ME-344 a promising candidate for cancer research.
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| ln Vitro |
ME-344 shows potent in vitro activity as an inhibitor of mitochondrial OXPHOS complex I. The compound exhibits anticancer activity by inhibiting cell growth and viability in leukemia cell lines with IC50 values of 70–260 nM. ME-344 disrupts ATP generation and oxygen consumption, leading to metabolic stress in cancer cells. The compound also downregulates the AKT/mTOR pathway, further contributing to its antiproliferative effects.
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| ln Vivo |
In vivo activity of ME-344 has been evaluated in preclinical models and clinical trials for the treatment of solid tumors. The compound has demonstrated significant bio-antitumor activity against HER2-negative breast cancer. ME-344 has been used in trials studying the treatment of solid tumors, indicating its potential for clinical development.
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| Enzyme Assay |
Non-cell-based enzyme assays for ME-344 typically involve measuring the inhibition of mitochondrial complex I activity using isolated mitochondria or purified complex I. A standard protocol includes: isolating mitochondria from tissue or cultured cells, incubating with complex I substrates (such as NADH and ubiquinone), and measuring NADH oxidation spectrophotometrically. ME-344 is added at various concentrations (0.001–100 μM), and the inhibition of NADH oxidation is monitored. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for ME-344 typically involve leukemia cell lines or other cancer cell lines. A representative protocol includes: culturing cells in appropriate medium, treating with ME-344 at various concentrations (0.01–100 μM) for 48–72 hours, and assessing cell viability using MTT or CellTiter-Glo assays. Mitochondrial function is assessed by measuring oxygen consumption rate (OCR) and extracellular acidification rate (ECAR) using a Seahorse analyzer. AKT/mTOR pathway inhibition is confirmed by Western blot.
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| Animal Protocol |
In vivo animal studies with ME-344 are conducted in xenograft mouse models of cancer, such as HER2-negative breast cancer xenografts. A typical protocol involves subcutaneous implantation of tumor cells in immunodeficient mice, allowing tumors to reach a certain size, administering ME-344 via oral gavage or intraperitoneal injection at doses determined from pharmacokinetic studies, monitoring tumor growth and body weight, and harvesting tumors for analysis of mitochondrial function and AKT/mTOR pathway modulation.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ME-344 have been characterized for in vivo administration. The compound has a molecular weight of 348.39 g/mol. ME-344 is soluble in DMSO at 70 mg/mL (200.92 mM) and in ethanol at 70 mg/mL, but is insoluble in water. In vivo formulation: 5% DMSO + 40% PEG300 + 5% Tween80 + 50% ddH2O (validated, solubility: 3.500 mg/mL) or 5% DMSO + 95% Corn oil (validated, solubility: 0.250 mg/mL).
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| Toxicity/Toxicokinetics |
As an investigational compound, ME-344 has been evaluated for safety in preclinical and clinical studies. The compound has been used in trials studying the treatment of solid tumors, indicating that safety data are available from clinical investigations. Standard safety assessments include cytotoxicity screening and toxicology studies in animal models. ME-344 is intended for research use only.
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| References | |
| Additional Infomation |
ME-344 has been used in clinical trials for the treatment of solid tumors. The mTOR1/2 kinase inhibitor ME-344 is the active metabolite of NV-128, a novel flavonoid small molecule inhibitor of the target of rapamycin (mTOR) with potential antitumor activity. After administration, the mTOR1/2 kinase inhibitor ME-344 downregulates the PIK3/AKT/mTOR pathway and causes chromatin condensation without caspase activation. Therefore, this drug can induce caspase-independent cell death in tumor cells or chemotherapy-resistant cells with dysregulated PIK3/AKT/mTOR pathways.
ME-344 (CAS 1374524-68-1) is a synthetic metabolite of NV-128 and a potent inhibitor of mitochondrial OXPHOS complex I, disrupting ATP generation and oxygen consumption. The compound also inhibits mTOR by downregulating the AKT/mTOR pathway, exhibiting anticancer activity in leukemia cell lines with IC50 values of 70–260 nM. ME-344 has been used in trials studying the treatment of solid tumors and has demonstrated significant bio-antitumor activity against HER2-negative breast cancer. |
| Molecular Formula |
C22H20O4
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|---|---|
| Molecular Weight |
348.39
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| Exact Mass |
348.136
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| CAS # |
1374524-68-1
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| PubChem CID |
68026984
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.419
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
453
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC1=C(C=CC2=C1OC[C@H]([C@H]2C3=CC=C(C=C3)O)C4=CC=C(C=C4)O)O
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| InChi Key |
QVCAATSEPLQVBX-FPOVZHCZSA-N
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| InChi Code |
InChI=1S/C22H20O4/c1-13-20(25)11-10-18-21(15-4-8-17(24)9-5-15)19(12-26-22(13)18)14-2-6-16(23)7-3-14/h2-11,19,21,23-25H,12H2,1H3/t19-,21-/m0/s1
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| Chemical Name |
(3R,4S)-3,4-bis(4-hydroxyphenyl)-8-methyl-3,4-dihydro-2H-chromen-7-ol
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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) |
Typically soluble in DMSO (e.g. 10 mM)
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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 | 2.8703 mL | 14.3517 mL | 28.7035 mL | |
| 5 mM | 0.5741 mL | 2.8703 mL | 5.7407 mL | |
| 10 mM | 0.2870 mL | 1.4352 mL | 2.8703 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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