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| Targets |
M-110 targets two distinct classes of enzymes: protein arginine N-methyltransferases (PRMTs) and the PIM kinase family. It is a potent and selective inhibitor of PIM kinases, with a strong preference for the PIM-3 isoform, exhibiting an IC50 of 0.047 μM for PIM-3, compared to 2.5 μM for both PIM-1 and PIM-2. The compound displays excellent selectivity in a panel of 261 kinases. By inhibiting PIM-3, M-110 reduces the expression of activated STAT3 (pSTAT3 Tyr705), a downstream effector in the PIM kinase signaling pathway.
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| ln Vitro |
The proliferation of DU-145 cells is inhibited by M-110 (0.01-10 μM; 72 hours) with an IC50 value of 0.9 μM [1]. Below 40 μM, M-110 exhibits no effect on normal human peripheral blood mononuclear cells [1]. STAT3 Tyr705 phosphorylation is inhibited by M-110 (10 μM; 18 hours) [1]. By suppressing PIM-3, M-110 reduces the expression of activated STAT3. Moreover, M-110 has IC50 values between 0.6 and 0.8 μM that prevent the growth of 22Rv1, PC3, and SW480 cells[1].
In vitro, M-110 demonstrates potent antiproliferative activity against various cancer cell lines. It inhibits the proliferation of DU-145 cells with an IC50 of 0.9 μM. It also inhibits the growth of 22Rv1, PC3, and SW480 cells with IC50 values between 0.6 and 0.8 μM. Importantly, M-110 shows no significant toxicity towards normal human peripheral blood mononuclear cells (PBMCs) at concentrations up to 40 μM, indicating a degree of selectivity for cancer cells. In mechanistic studies, treatment with 10 μM M-110 for 18 hours reduces p-STAT3 (Tyr705) expression to 23.5% of untreated control levels without affecting total STAT3 expression. |
| ln Vivo |
Specific in vivo activity data for M-110 are not extensively documented in the available literature. As a research compound primarily used in cell-based assays to study cancer biology, its in vivo efficacy and pharmacokinetic properties remain to be fully characterized. However, based on its potent in vitro activity against prostate and other cancer cell lines, M-110 is expected to show antitumor effects in appropriate animal models. Such studies would typically involve administration via oral gavage or intraperitoneal injection to evaluate tumor growth inhibition and overall survival in xenograft models.
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| Enzyme Assay |
For in vitro enzyme assays, M-110 is typically dissolved in DMSO and tested at various concentrations against purified PRMT or PIM kinase enzymes. Kinase activity is measured by quantifying the phosphorylation of peptide substrates using radiolabeled ATP or fluorescence-based detection methods. IC50 values are calculated from dose-response curves. For selectivity profiling, the compound is tested against a broad panel of kinases to assess its off-target effects.
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| Cell Assay |
Cell viability assay [1]
Cell Types: DU-145 cells Tested Concentrations: 0.01, 0.1, 1, 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibits DU-145 cell growth, IC50 value is 0.9 μM. Western Blot Analysis [1] Cell Types: DU-145 Cell Tested Concentrations: 10 μM Incubation Duration: 18 hrs (hours) Experimental Results: Compared with untreated cells, the expression of p-STAT3 Tyr705 was diminished to 23.5% without affecting the expression of STAT3. In vitro cellular assays are performed using cancer cell lines such as DU-145, 22Rv1, PC3, and SW480. Cells are cultured in appropriate media at 37°C in a 5% CO₂ incubator. M-110, dissolved in DMSO, is added to the culture medium at various concentrations (e.g., 0.01-10 μM) and incubated for 72 hours. Cell viability is assessed using standard assays like MTT or CellTiter-Glo to determine IC50 values. For mechanistic studies, cells are treated with M-110 (e.g., 10 μM for 18 hours), and protein expression is analyzed by Western blot. |
| Animal Protocol |
In vivo animal studies for M-110 would be conducted in murine xenograft models using human cancer cell lines, such as DU-145 or PC3 prostate cancer cells. M-110 would be administered via oral gavage or intraperitoneal injection at various doses. Endpoints would include tumor growth inhibition, measured by caliper, as well as survival analysis. Pharmacokinetic studies would be conducted to determine plasma concentrations, half-life, and bioavailability. Histopathological analysis of tumors and other tissues would be performed to assess efficacy and potential toxicity.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic parameters for M-110 are not extensively documented in the available literature. As a small molecule with a molecular weight of 445.95 and a LogP of 4.08, it is expected to have reasonable cell permeability and oral bioavailability, characteristics typical of kinase inhibitors. The compound is soluble in DMSO and is typically stored as a powder at -20°C. Further studies are needed to fully characterize its absorption, distribution, metabolism, and excretion (ADME) properties.
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| Toxicity/Toxicokinetics |
Specific toxicity data for M-110 are limited. However, in vitro studies indicate that the compound shows no effect on normal human peripheral blood mononuclear cells (PBMCs) at concentrations up to 40 μM, suggesting a favorable safety profile in terms of selectivity for cancer cells. Standard laboratory safety precautions should be followed when handling this compound. It is intended for research use only and not for human therapeutic applications.
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| References |
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| Additional Infomation |
M-110 is a research compound used to study the role of PRMTs and PIM kinases in cancer. Its dual inhibitory activity against both PRMTs and the PIM kinase family makes it a valuable tool for investigating the interplay between these two important oncogenic pathways. By inhibiting PIM kinases, particularly PIM-3, M-110 reduces the phosphorylation of STAT3 at Tyr705, a key signaling node in many cancers. It is commercially available from various suppliers for research purposes only.
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| Molecular Formula |
C22H28CLN5O3
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| Molecular Weight |
445.95
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| Exact Mass |
445.188
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| CAS # |
1395048-49-3
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| PubChem CID |
136639479
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.623
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| LogP |
4.08
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
31
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| Complexity |
588
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC/C(=N/NC(=O)C1=CC(=NC=C1)NCCCN2CCOCC2)/C3=C(C=C(C=C3)Cl)O
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| InChi Key |
FXXCNYVQIONABS-XHPQRKPJSA-N
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| InChi Code |
InChI=1S/C22H28ClN5O3/c1-2-19(18-5-4-17(23)15-20(18)29)26-27-22(30)16-6-8-25-21(14-16)24-7-3-9-28-10-12-31-13-11-28/h4-6,8,14-15,29H,2-3,7,9-13H2,1H3,(H,24,25)(H,27,30)/b26-19-
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| Chemical Name |
N-[(Z)-1-(4-chloro-2-hydroxyphenyl)propylideneamino]-2-(3-morpholin-4-ylpropylamino)pyridine-4-carboxamide
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| Synonyms |
M110 M 110 M-110
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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 : ~33.33 mg/mL (~74.74 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.61 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 25.0 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 (4.66 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 | 2.2424 mL | 11.2120 mL | 22.4240 mL | |
| 5 mM | 0.4485 mL | 2.2424 mL | 4.4848 mL | |
| 10 mM | 0.2242 mL | 1.1212 mL | 2.2424 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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