MT-125 free base
Based on 1 Customer Validation
MT-125 free base is a specific and well-tolerated inhibitor of non-muscle myosin IIA (Ki,NMIIA = 2.7 μM) and IIB (EC50 = 1.7 μM). MT-125 free base can pass through the blood-brain barrier. MT-125 free base induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 free base can enhance the PDGFR signaling pathway. MT-125 free base can be used for research on glioblastoma.
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- Purity : 98.67%
- CAS No.: 2404652-80-6
- 화학식: C22H19N3O2
- 분자량:357.41
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
PDGFRα |
In Vitro
MT-125 free base (5 μM, 8 h) significantly inhibits the invasive ability of one murine (MES1861) and three human (187, 190, and L1) Glioblastoma (GBM) cell lines[1].
MT-125 free base (5 μM, 48 h) leads to 12 %-25 % cell multinucleation in 10 human GBM cells[1].
MT-125 free base (0.1-10 μM; 96 h) produces over 90 % cytotoxicity in various mouse and human GBM cell lines[1].
MT-125 increase reactive oxygen species (ROS) and lipid peroxidation levels in L1 cells[1].
MT-125 free base (4 μM) can induce ferroptosis and ferroptosis inhibitors can reverse its cytotoxicity in Trp53(-/-) cells[1].
MT-125 free base (5 μM, 48 h) significantly increase PDGFRα expression and activation of downstream signaling pathways in Trp53(-/-) cells[1].
MT-125 free base (5 μM, 48 h) regulates the MAPK signaling pathway by inhibiting NMIIA in Trp53(-/-) cells[1].
MT-125 free base (5 μM, 48 h) exhibits synergistic effects with carcinogenic kinase inhibitors in Trp53(-/-) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:murine (TRP53(-/-), Pten(-/-), TRP53/Pten(-/-)) and human (L1, L0, GBM1A, 612, QNS120, QNS166, QNS315) GBM cell lines
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Concentration:3.3-7.3 μM
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Incubation Time:96 h
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Result:Significantly inhibited the GBM cell lines.
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Cell Line:Trp53(‒/‒) cells
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Concentration:5 μM
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Incubation Time:48 h
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Result:Effectively enhanced activation of PDGFRα, AKT, mTOR, ERK1/2, and SRC.
In Vivo
MT-125 free base (20 mg/kg, s.c.; once daily; for 7 days) does not cause any adverse effects related to medication and does not affect age-related weight changes in the C57BL/6 mice[1].
MT-125 free base (7.5, 15, or 30 mg/kg; s.c.; once daily; for 28 days) maintain good tolerability in repeated dose toxicology studies in the female rats[1].
MT-125 free base (10 mg/kg; i.p.; once daily; for 4 weeks) synergizes with oncogenic kinase inhibitors and can significantly inhibit the growth of tumor cells in the C57BL/6 mice with Trp53(?/?) tumors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (8-10 weeks; 25-35 g)[1]
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Dosage:10 mg/kg
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Administration:Subcutaneous injection (s.c.); once daily for 2 weeks
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Result:Had good tolerance and the weight and hematological indicators of mice were within normal range.
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Animal Model:C57BL/6 mice (8-10 weeks; 25-35 g)[1]
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Dosage:20 mg/kg
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Administration:Subcutaneous injection (s.c.); once daily for 7 days
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Result:Maintained normal body weight and hematological parameters within the normal range in mice.
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Animal Model:Female rats (8-10 weeks; 25-35 g)[1]
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Dosage:7.5, 15, or 30 mg/kg
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Administration:Subcutaneous injection (s.c.); once daily for 28 days
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Result:Did not cause any obvious or lasting adverse health effects.
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Animal Model:C57BL/6 mice with Trp53(‒/‒) tumors (8-10 weeks; 25-35 g)[1]
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Dosage:10 mg/kg, co-incubation with Paxalisib (HY-19962)
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Administration:Intraperitoneal injection (i.p.); once daily for 4 weeks
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Result:Markedly reduced tumor size to an isolated nest of HA-positive cells and prolonged survival rate.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2404652-80-6
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Appearance Solid
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분자량 357.41
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화학식 C22H19N3O2
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Color Light yellow to yellow
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SMILES
CC1=CC2=C(N=C(N(C3=CC4=C(N=C(C)C=C4)C=C3)CC5)[C@]5(O)C2=O)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
In Vitro:
DMSO : 33.33 mg/mL (93.25 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 3.33 mg/mL (9.32 mM); Clear solution
This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Protocol
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Ferroptosis Solutions
Ferroptosis is an iron-dependent, non-apoptotic form of regulated cell death characterized by lethal lipid peroxidation and sensitivity to suppression by iron chelators or lipophilic radical-trapping antioxidants. The core pathway links cystine uptake through system Xc−, glutathione availability, GPX4-dependent detoxification of phospholipid hydroperoxides, iron-dependent oxidative reactions, and polyunsaturated-phospholipid metabolism into a cell-death program that is biochemically and morphologically distinct from apoptosis, necrosis, and autophagy. The ferroptosis pathway is experimentally linked to phenotype through chemical and genetic perturbation. Erastin induces ferroptosis by inhibiting cystine uptake through system Xc− and weakening antioxidant defenses, while GPX4 inhibition or depletion causes lipid peroxide accumulation and ferroptotic cancer-cell death. ACSL4 and oxidizable arachidonoyl- or adrenoyl-containing phosphatidylethanolamines shape ferroptosis sensitivity by con
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
순도&문서
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Data Sheet (285 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7979 mL | 13.9895 mL | 27.9791 mL | 69.9477 mL |
| 5 mM | 0.5596 mL | 2.7979 mL | 5.5958 mL | 13.9895 mL | |
| 10 mM | 0.2798 mL | 1.3990 mL | 2.7979 mL | 6.9948 mL | |
| 15 mM | 0.1865 mL | 0.9326 mL | 1.8653 mL | 4.6632 mL | |
| 20 mM | 0.1399 mL | 0.6995 mL | 1.3990 mL | 3.4974 mL | |
| 25 mM | 0.1119 mL | 0.5596 mL | 1.1192 mL | 2.7979 mL | |
| 30 mM | 0.0933 mL | 0.4663 mL | 0.9326 mL | 2.3316 mL | |
| 40 mM | 0.0699 mL | 0.3497 mL | 0.6995 mL | 1.7487 mL | |
| 50 mM | 0.0560 mL | 0.2798 mL | 0.5596 mL | 1.3990 mL | |
| 60 mM | 0.0466 mL | 0.2332 mL | 0.4663 mL | 1.1658 mL | |
| 80 mM | 0.0350 mL | 0.1749 mL | 0.3497 mL | 0.8743 mL |
MT-125 free base Related Classifications
HY-174406A Related Classifications
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