| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
MST-312 targets telomerase, the enzyme responsible for maintaining telomere length in cells. Telomerase is a ribonucleoprotein reverse transcriptase that adds telomeric repeats to chromosome ends, preventing telomere shortening and cellular senescence. Telomerase is highly active in cancer cells but largely inactive in normal somatic cells, making it an attractive target for cancer therapy. MST-312 inhibits telomerase activity with an IC50 of 0.67 μM in a TRAP assay. As a chemically modified derivative of EGCG, MST-312 has improved stability and potency compared to the parent compound. By inhibiting telomerase, MST-312 induces telomere shortening, leading to cellular senescence or apoptosis in cancer cells.
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| ln Vitro |
Cell viability is decreased by MST-312 (2~8 μM; 0~72 hours; U-266 cells) in a dose- and time-dependent way [1]. Inducing cellular antagonists, MST-312 (2~8 μM; 48 hours; U-266 cells) suppresses c-Myc and hTERT cells, inhibits the pro-gene Bax, and antagonizes the anti-liver cancer gene Bcl-2 [1].
MST-312 is a telomerase inhibitor with an IC50 of 0.67 μM in a TRAP assay. The compound exhibits antineoplastic activity. It is a chemically modified derivative of green tea epigallocatechin gallate (EGCG) with improved stability and potency. MST-312 can be used for the research of cancer, such as multiple myeloma (MM). Combination treatment with morin and MST-312 reduces cancer stem cell traits by targeting STAT3 and telomerase. |
| ln Vivo |
In vivo, MST-312 has been studied in animal models of cancer, particularly multiple myeloma. The compound's ability to inhibit telomerase and induce telomere shortening may lead to tumor growth inhibition. MST-312 can be used in combination with other therapeutic agents to enhance antitumor efficacy. The compound's improved stability compared to EGCG supports its use in in vivo studies. It has been studied for the treatment of various cancers including multiple myeloma and other malignancies.
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| Enzyme Assay |
Telomerase activity assays for MST-312 are performed using the TRAP (telomeric repeat amplification protocol) assay. Cell lysates containing telomerase are incubated with a telomerase substrate primer in the presence of dNTPs and varying concentrations of MST-312. Telomerase extends the primer by adding telomeric repeats, and the extended products are amplified by PCR. The PCR products are separated by gel electrophoresis and quantified. IC50 values are calculated from concentration-response curves. The assay measures the inhibition of telomerase activity by MST-312.
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: U-266 cells Tested Concentrations: 2~8 μM Incubation Duration: 0~72 hrs (hours) Experimental Results: The viability of U-266 cells is dose-dependent and gene expression [1]. Response to MST-312 exposure in a time-dependent manner. Apoptosis analysis [1] Cell Types: U-266 cells Tested Concentrations: 2~8 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induced apoptosis in a dose-dependent manner. RT-PCR[1] Cell Types: U-266 Cell Tested Concentrations: 2 μM Incubation Duration: 48 hrs (hours) Experimental Results: Up-regulated the pro-apoptotic gene Bax, down-regulated the expression of the anti-apoptotic gene Bcl-2, and inhibited the c-Myc and hTERT genes. Cellular assays for telomerase inhibition typically employ cancer cell lines with high telomerase activity, such as multiple myeloma cells (e.g., MM cell lines). Cells are treated with varying concentrations of MST-312 for 1-14 days. Telomerase activity is assessed using the TRAP assay in cell lysates. Telomere length is measured by Southern blot or telomere-specific qPCR. Cell proliferation is assessed by MTT or CellTiter-Glo assays. Apoptosis is evaluated by Annexin V/PI staining. Cellular senescence is assessed by β-galactosidase staining. The compound's effects on cancer stem cell traits can be assessed by sphere formation assays. |
| Animal Protocol |
In vivo efficacy is evaluated in mouse xenograft models using human cancer cell lines, particularly multiple myeloma cells. Tumor-bearing mice are treated with MST-312 (typically administered intraperitoneally or orally) at various doses. Tumor volumes are measured every 2-3 days. Telomerase activity and telomere length are measured in tumor tissues. The compound's effects on tumor growth, apoptosis, and senescence are assessed by histology and immunohistochemistry. Combination studies with other therapeutic agents are conducted to assess synergistic efficacy.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for MST-312 are limited. The compound is a chemically modified derivative of EGCG with improved stability. It is soluble in DMSO and other organic solvents. The compound should be stored at -20°C for long-term stability. For in vivo studies, appropriate formulations would be required. Standard pharmacokinetic studies would be needed for any therapeutic development.
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| Toxicity/Toxicokinetics |
Toxicological data for MST-312 are limited as it is a research compound. As a telomerase inhibitor, potential toxicities may include effects on telomerase-positive stem cells and germ cells, although telomerase is largely inactive in normal somatic cells. The compound should be handled with appropriate laboratory safety precautions. In preclinical studies, MST-312 has been evaluated with acceptable tolerability at the doses used. Standard safety pharmacology studies would be required for clinical development.
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| References | |
| Additional Infomation |
N-[3-[[(2,3-dihydroxyphenyl)-oxymethyl]amino]phenyl]-2,3-dihydroxybenzamide is a member of the benzamide class of compounds.
MST-312 is a telomerase inhibitor and a chemically modified derivative of green tea epigallocatechin gallate (EGCG). It is also known as Telomerase Inhibitor IX. The compound has an IC50 of 0.67 μM in a TRAP assay. It exhibits antineoplastic activity and can be used for the research of cancer, such as multiple myeloma (MM). Combination treatment with morin and MST-312 reduces cancer stem cell traits by targeting STAT3 and telomerase. |
| Molecular Formula |
C20H16N2O6
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| Molecular Weight |
380.35084
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| Exact Mass |
380.101
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| CAS # |
368449-04-1
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| PubChem CID |
10385095
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| Appearance |
White to off-white solid powder
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| LogP |
3.781
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
513
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MIQUEZGHEJGPJB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H16N2O6/c23-15-8-2-6-13(17(15)25)19(27)21-11-4-1-5-12(10-11)22-20(28)14-7-3-9-16(24)18(14)26/h1-10,23-26H,(H,21,27)(H,22,28)
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| Chemical Name |
N-[3-[(2,3-dihydroxybenzoyl)amino]phenyl]-2,3-dihydroxybenzamide
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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 : ~125 mg/mL (~328.64 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.75 mg/mL (9.86 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 37.5 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: 3.75 mg/mL (9.86 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 37.5 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. View More
Solubility in Formulation 3: ≥ 3.75 mg/mL (9.86 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6292 mL | 13.1458 mL | 26.2916 mL | |
| 5 mM | 0.5258 mL | 2.6292 mL | 5.2583 mL | |
| 10 mM | 0.2629 mL | 1.3146 mL | 2.6292 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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