M-110
Based on 1 Customer Validation
M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.
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- Purity: 99.05%
- CAS No.: 1395048-49-3
- 화학식: C22H28ClN5O3
- 분자량:445.94
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
M-110 (0.01-10 μM; 72 hours) inhibiting the growth of DU-145 cells with an IC50?value of 0.9 μM[1]. M-110 has no activity on normal human peripheral blood mononuclear cells up to 40 μM[1].
M-110 (10 μM; 18 hours) inhibits STAT3 Tyr705?phosphorylation[1].
M-110 inhibits the expression of active STAT3 through inhibition of PIM-3. M-110 also inhibits the proliferation of 22Rv1, PC3, and SW480 cells, with IC50?values of 0.6 to 0.8 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DU-145 cells
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Concentration:0.01, 0.1, 1, 10 μM
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Incubation Time:72 hours
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Result:Inhibiting the growth of DU-145 cells with an IC50 value of 0.9 μM.
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Cell Line:DU-145 cells
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Concentration:10 μM
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Incubation Time:18 hours
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Result:Reduced the expression of p-STAT3 Tyr705 to 23.5%, compared with untreated cells without affecting the expression of STAT3.
Chemical Information
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CAS No. 1395048-49-3
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Appearance Solid
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분자량 445.94
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화학식 C22H28ClN5O3
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Color Light yellow to yellow
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SMILES
O=C(N/N=C(C1=CC=C(Cl)C=C1O)\CC)C2=CC(NCCCN3CCOCC3)=NC=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
In Vitro:
DMSO : 33.33 mg/mL (74.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.66 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Chang M, et al.PIM kinase inhibitors downregulate STAT3(Tyr705) phosphorylation.Mol Cancer Ther. 2010 Sep;9(9):2478-87. [Content Brief]
[2]. He Y, et al. Schisantherin A suppresses osteoclast formation and wear particle-induced osteolysis via modulating RANKL signaling pathways. Biochem Biophys Res Commun. 2014 Jul 4;449(3):344-50. [Content Brief]
[3]. Zhou E, et al. Schisantherin A protects lipopolysaccharide-induced acute respiratory distress syndrome in mice through inhibiting NF-κB and MAPKs signaling pathways. Int Immunopharmacol. 2014 Sep;22(1):133-40. [Content Brief]
[4]. Sa F, et al. Discovery of novel anti-parkinsonian effect of schisantherin A in in vitro and in vivo. Neurosci Lett. 2015 Apr 23;593:7-12. [Content Brief]
[5]. Zhang LQ, et al. Schisantherin A protects against 6-OHDA-induced dopaminergic neuron damage in zebrafish and cytotoxicity in SH-SY5Y cells through the ROS/NO and AKT/GSK3β pathways. J Ethnopharmacol. 2015 Apr 29. pii: S0378-8741(15)00306-2. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.2425 mL | 11.2123 mL | 22.4245 mL | 56.0614 mL |
| 5 mM | 0.4485 mL | 2.2425 mL | 4.4849 mL | 11.2123 mL | |
| 10 mM | 0.2242 mL | 1.1212 mL | 2.2425 mL | 5.6061 mL | |
| 15 mM | 0.1495 mL | 0.7475 mL | 1.4950 mL | 3.7374 mL | |
| 20 mM | 0.1121 mL | 0.5606 mL | 1.1212 mL | 2.8031 mL | |
| 25 mM | 0.0897 mL | 0.4485 mL | 0.8970 mL | 2.2425 mL | |
| 30 mM | 0.0747 mL | 0.3737 mL | 0.7475 mL | 1.8687 mL | |
| 40 mM | 0.0561 mL | 0.2803 mL | 0.5606 mL | 1.4015 mL | |
| 50 mM | 0.0448 mL | 0.2242 mL | 0.4485 mL | 1.1212 mL | |
| 60 mM | 0.0374 mL | 0.1869 mL | 0.3737 mL | 0.9344 mL |
M-110 Related Classifications
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