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| Targets |
MP7 targets phosphoinositide-dependent kinase-1 (PDK1), a serine/threonine kinase that phosphorylates the activation loop of AGC kinases such as AKT/PKB, SGK, and RSK. By inhibiting PDK1, MP7 reduces the phosphorylation and activation of these downstream kinases, thereby disrupting cell survival and proliferation signaling pathways. PDK1 is a key node in the PI3K/AKT pathway, which is frequently dysregulated in cancer.
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| ln Vitro |
Alisertib and MP7 (PDK1 first step) were able to decrease the number of viable cells in short sequences, as shown by cell counting of U87MG-derived neuroastromatoma stem cells (GSC). GSC was employed at the greatest dosages (i.e., 1.5 μM Alisertib and 2.5 μM MP7), as reported in U87MG cells, and when combined, compared to treatment of single cells, produced a considerable increase in the number of dead cells. After therapy for 72 hours, MP7 by itself did not significantly reduce the growth of pleomorphic astroblastoma (GBM). It has been demonstrated that MP7, with IC50 values in the micromolar range, influences the fold development of monolayer cells in a spectrum of astroblastomas [1].
In vitro studies demonstrate that MP7 is able to decrease the number of viable cells. In U87MG cells, MP7 reduces cell viability. However, MP7 has been shown to have only minimal effects on monolayer cell growth in several cancer cell lines, with IC₅0 values in the micromolar range. When used together with other compounds, MP7 can further reduce the activity of glioblastoma stem cells (GSCs) compared to单独 treatment. |
| ln Vivo |
In vivo activity of MP7 has not been extensively characterized in the available literature. As a PDK1 inhibitor, the compound has potential applications in cancer research, particularly for targeting tumors with dysregulated PI3K/AKT signaling. However, detailed in vivo efficacy data, including tumor growth inhibition in xenograft models, are not extensively reported. The compound is primarily used as a research tool for in vitro studies of PDK1 signaling.
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| Enzyme Assay |
In vitro enzyme assays for MP7 involve measuring its inhibition of PDK1 kinase activity. The assay typically uses purified recombinant PDK1 enzyme, a peptide substrate (e.g., AKT-derived peptide), and ATP. The compound is incubated with the enzyme and substrates, and phosphorylation is quantified by scintillation counting using radiolabeled ATP or by ELISA. IC₅0 values are calculated from dose-response curves. Selectivity profiling may be performed using panels of other kinases to assess the compound's specificity for PDK1.
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| Cell Assay |
Cellular assays for MP7 are conducted using cancer cell lines to evaluate its effects on PDK1 signaling, cell viability, and proliferation. Cells are treated with varying concentrations of the compound (typically 1-100 microM) for 24-72 hours. PDK1 activity is assessed by measuring the phosphorylation of downstream targets such as AKT (p-AKT) by Western blotting. Cell viability is assessed using MTT, CCK-8, or CellTiter-Glo assays. The compound's effects on cell proliferation and apoptosis are evaluated using standard assays.
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| Animal Protocol |
In vivo animal studies for MP7 are limited, as the compound is primarily used as a research tool. For in vivo efficacy studies, xenograft models using cancer cell lines could be employed. Tumor-bearing mice would be treated with the compound via intraperitoneal or oral administration at various doses. Tumor volume would be measured regularly, and body weight monitored for tolerability. At study termination, tumors would be analyzed for PDK1 signaling markers and apoptosis. However, specific in vivo study protocols and results are not extensively reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MP7 have been partially characterized. The compound has a molecular weight of 516.50 and a molecular formula of C2₈H22F2N4O4. It is soluble in DMSO at ≥100 mg/mL (193.61 mM) but has poor aqueous solubility (<0.1 mg/mL in water). The compound is available in high purity (>98%). Detailed PK parameters such as half-life, bioavailability, and volume of distribution are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
Toxicological data for MP7 are limited, as the compound is used primarily as a research tool. The compound is not intended for human therapeutic use and is supplied for research purposes only. In cell-based assays, the compound is generally well-tolerated at concentrations used for PDK1 inhibition studies. Higher concentrations may cause non-specific effects or cytotoxicity. Standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
MP7 is a PDK1 inhibitor used as a research tool for studying the PDK1 signaling pathway and its role in cancer and other diseases. It is a small molecule inhibitor with a molecular weight of 516.50 and a molecular formula of C2₈H22F2N4O4. The compound is not an FDA-approved drug and has no clinical indications. It is available in high purity (>98%) and is typically stored at -20degC. The compound is soluble in DMSO but has poor aqueous solubility.
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| Molecular Formula |
C28H22N4O4F2
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|---|---|
| Molecular Weight |
516.49548
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| Exact Mass |
516.16
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| CAS # |
1001409-50-2
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| PubChem CID |
56965967
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
724.4±60.0 °C at 760 mmHg
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| Flash Point |
391.9±32.9 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.640
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| LogP |
3.32
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
38
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| Complexity |
953
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GCWCGSPBENFEPE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H22F2N4O4/c29-21-10-8-17(13-22(21)30)15-34-12-4-7-20(27(34)36)26(35)31-25(18-5-2-1-3-6-18)16-38-19-9-11-23-24(14-19)33-28(37)32-23/h1-14,25H,15-16H2,(H,31,35)(H2,32,33,37)
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| Chemical Name |
1-[(3,4-difluorophenyl)methyl]-2-oxo-N-[2-[(2-oxo-1,3-dihydrobenzimidazol-5-yl)oxy]-1-phenylethyl]pyridine-3-carboxamide
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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 : ≥ 100 mg/mL (~193.61 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (5.32 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 27.5 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: ≥ 2.75 mg/mL (5.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 27.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9361 mL | 9.6805 mL | 19.3611 mL | |
| 5 mM | 0.3872 mL | 1.9361 mL | 3.8722 mL | |
| 10 mM | 0.1936 mL | 0.9681 mL | 1.9361 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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