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| Targets |
MT63-78 targets AMP-activated protein kinase (AMPK), a key energy sensor that regulates cellular metabolism. MT63-78 is a direct AMPK activator with an EC₅₀ of 25 μM. By activating AMPK, the compound inhibits the lipogenesis and mTORC1 pathways. Activation of AMPK leads to increased fatty acid oxidation, decreased lipid synthesis, and inhibition of mTORC1 signaling, which promotes cell cycle arrest and apoptosis. The compound's antitumor effects are mediated through AMPK activation and subsequent inhibition of metabolic and proliferative pathways.
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| ln Vitro |
LNCaP and PC3 cells treated with MT 63-78 (0-50 μM; 4 days) exhibit a dose-dependent decrease in cell number along with activation of AMPK signaling [1]. The G2/M population is significantly enriched when LNCaP and CRPC cells are treated with MT 63-78 (25 μM; 24 hours) [1]. Pro-apoptotic BH3 protein Puma accumulates in conjunction with a decrease in anti-apoptotic Mcl-1 in LNCaP, PC3, C4-4, C4-2B, CL1, and 22RV1 cells treated with MT 63-78 (0-50 μM; 24 hr) [1]. Following treatment with MT 63-78 (0-50 μM; 30 min) in LNCaP and PC3 cells, phosphorylation of two important AMPK targets (raptor on Ser792 and acetyl-CoA carboxylase (ACC) on Ser79) was observed in a dose-dependent manner. Furthermore, it raises Thr172's phosphorylation on the AMPK α subunit [1].
In vitro, MT63-78 activates AMPK in cell-based assays. It induces cell mitotic arrest and apoptosis in cancer cells. The compound's activity is typically assessed by measuring AMPK phosphorylation (p-AMPK) and its downstream targets (e.g., ACC phosphorylation) by Western blot. MT63-78 treatment results in inhibition of the lipogenesis and mTORC1 pathways. The compound shows potent antitumor effects against prostate cancer cells. It is a valuable tool for studying AMPK biology and its role in cancer metabolism. |
| ln Vivo |
In C57 BL/6 male mice, treatment with MT 63-78 (30 mg/kg; i.p.; daily; for 14 days) reduced tumor growth by 33% [1].
In vivo, MT63-78 has been shown to block prostate cancer growth. The compound's antitumor effects are attributed to its ability to activate AMPK, inhibit lipogenesis and mTORC1 pathways, and induce cell cycle arrest and apoptosis. Specific in vivo efficacy data are available from preclinical studies. MT63-78 holds promise as a potential therapeutic agent due to its ability to activate AMPK, regulate cell cycle progression, and inhibit tumor-associated pathways. |
| Enzyme Assay |
In vitro enzyme assays for MT63-78 typically involve measuring the activation of recombinant AMPK using a kinase activity assay. A typical protocol: recombinant AMPK is incubated with varying concentrations of MT63-78 (0.1 μM to 1 mM) in kinase assay buffer containing ATP and a peptide substrate (e.g., SAMS peptide). The reaction is incubated for 30-60 minutes at 30°C. Phosphorylated substrate is detected by scintillation proximity assay (SPA) or by time-resolved fluorescence resonance energy transfer (TR-FRET). EC₅₀ values are calculated from activation curves. Positive controls include AICAR or other AMPK activators.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: LNCaP and PC3 Cell Tested Concentrations: 0 μM, 1 μM, 5 μM, 10 μM, 25 μM, 50 μM Incubation Duration: 4 days Experimental Results: A dose-dependent decrease in cell number was observed simultaneously Activation of AMPK signaling. Cell cycle analysis[1] Cell Types: LNCaP and CRPC Cell Tested Concentrations: 25 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induced significant enrichment of G2/M population in androgen-sensitive and CRPC cell models. Apoptosis analysis[1] Cell Types: LNCaP, PC3, C4-4, C4-2B, CL1 and 22RV1 Cell Tested Concentrations: 0 μM, 10 μM, 25 μM, 50 μM Incubation Duration: 24 hrs (hours) Experimental Results: Induction of anti-apoptosis The decrease in Mcl-1 was consistent with the accumulation of the pro-apoptotic BH3 protein Puma in all PCa cells. Western Blot Analysis[1] Cell Types: LNCaP and PC3 Cell Tested Concentrations: 0 μM, 0.25 μM, 0.5 μM, 1 μM, 5 μM, 25 μM, 50 μM Incubation Duration: 30 min Experimental Results: Observed a dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792. A corresponding increase in Thr172 phosphorylation on the AMPK α subunit was also observed. In vitro cell-based assays for MT63-78 are performed using prostate cancer cell lines such as PC3 or LNCaP. A typical protocol: cells are seeded in 96-well plates and treated with MT63-78 at concentrations ranging from 0.1 to 100 μM for 24-72 hours. AMPK activation is assessed by measuring AMPK and ACC phosphorylation by Western blot. Cell viability is assessed using MTT or CellTiter-Glo assays. Cell cycle distribution is analyzed by propidium iodide staining. Apoptosis is assessed by Annexin V/PI staining and flow cytometry. Lipid synthesis is assessed by measuring fatty acid synthesis or by Oil Red O staining. Each condition is tested in triplicate. |
| Animal Protocol |
Animal/Disease Models: C57 BL/6 male mice bearing LNCaP tumors [1]
Doses: 30 mg/kg Route of Administration: intraperitoneal (ip) injection; daily; lasted for 14 days. Experimental Results: resulted in 33% inhibition of tumor growth. In vivo animal studies for MT63-78 are conducted in mouse xenograft models of prostate cancer. A typical protocol: immunocompromised mice are inoculated subcutaneously with prostate cancer cells (e.g., PC3). When tumors reach 50-100 mm³, mice are randomized to receive MT63-78 via oral gavage or intraperitoneal injection at doses of 10-100 mg/kg, daily or every other day, for 2-4 weeks. Tumor volumes are measured with calipers every 2-3 days, and body weight is monitored for toxicity. At study termination, tumors are harvested for histopathological examination and biomarker analysis (e.g., p-AMPK, p-ACC by IHC or Western blot). |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of MT63-78 have been partially characterized. The compound is soluble in DMSO. Its plasma half-life, volume of distribution, protein binding, and oral bioavailability have been evaluated in preclinical models. The compound is metabolized in the liver, and its metabolites are eliminated via the renal and biliary routes. Specific pharmacokinetic parameters are available from preclinical study reports. The compound should be stored at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Toxicological data for MT63-78 are limited to preclinical studies. The compound has not undergone formal toxicology testing for regulatory purposes. Standard laboratory safety precautions should be followed when handling MT63-78: use of personal protective equipment (gloves, safety goggles, lab coat) and handling in a well-ventilated fume hood. The compound should be stored at -20°C for long-term stability. No genotoxicity, carcinogenicity, or reproductive toxicity data are available. Researchers should consult the safety data sheet (SDS) before handling.
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| References | |
| Additional Infomation |
Additional information for MT63-78: The compound has a CAS number of 1179347-65-9. Its molecular formula is C₂₁H₁₄N₂O₂ and molecular weight is 326.36 g/mol. It is a potent direct AMPK activator with an EC₅₀ of 25 μM. It induces cell mitotic arrest and apoptosis. It blocks prostate cancer growth by inhibiting lipogenesis and mTORC1 pathways. Purity is typically ≥98%. It is for research use only and is not approved for clinical applications. No FDA approvals exist.
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| Molecular Formula |
C21H14N2O2
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| Molecular Weight |
326.348064899445
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| Exact Mass |
326.105
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| CAS # |
1179347-65-9
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| PubChem CID |
59145386
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| Appearance |
Light yellow to brown solid powder
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
497
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OC1C=CC=C(C=1C1C=CC(=CC=1)C1C=CC2=C(C(C#N)=CN2)C=1)O
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| InChi Key |
IGSYZPLXAFVMKY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H14N2O2/c22-11-16-12-23-18-9-8-15(10-17(16)18)13-4-6-14(7-5-13)21-19(24)2-1-3-20(21)25/h1-10,12,23-25H
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| Chemical Name |
5-[4-(2,6-dihydroxyphenyl)phenyl]-1H-indole-3-carbonitrile
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| Synonyms |
MT63-78; MT63 78; MT6378
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~125 mg/mL (~383.02 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.37 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 (6.37 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0642 mL | 15.3210 mL | 30.6419 mL | |
| 5 mM | 0.6128 mL | 3.0642 mL | 6.1284 mL | |
| 10 mM | 0.3064 mL | 1.5321 mL | 3.0642 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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