TMLZ-G46
Based on 1 Customer Validation
TMLZ-G46 is an orally active ZNF207 inhibitor with blood-brain barrier penetration ability, with a Kd value of 68 nM. TMLZ-G46 inhibits cancer cell proliferation, stemness, migration and invasion, induces G0/G1 cell cycle arrest and apoptosis, and suppresses colony formation. TMLZ-G46 can be used in glioma research.
For research use only. We do not sell to patients.
- Purity : 98.45%
- CAS No.: 3116767-83-7
- Formula: C37H41N3O3
- Molecular Weight:575.74
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
TMLZ-G46 (10 μM; 3 h) binds to ZNF207 in LN229 and U251MG glioma cells, and significantly increases the thermal stability of this protein[1].
TMLZ-G46 (72 h) potently inhibits the proliferation of glioma cell lines with high ZNF207 expression (LN229, U251MG, HS683, T98G), with IC50 values below 3 μM, while its activity decreases in cell lines with low ZNF207 expression (U87MG, U118MG, U138MG)[1].
TMLZ-G46 (0.25-4 μM; 14 days) potently impairs the clonogenic capacity of LN229 and U251MG glioma cells, with significant inhibitory effects observable at concentrations as low as 0.25 μM[1].
TMLZ-G46 (10 days) selectively inhibits the self-renewal of glioma stem-like cells in LN229 and U251MG cells, with an IC50 value at the submicromolar level[1].
TMLZ-G46 (0.5-4 μM; 24 h) dose-dependently inhibits the expression of SOX2 in LN229 and U251MG glioma cells, providing a basis for its inhibition of stem cell properties[1].
TMLZ-G46 (0-8 μM; 24-48 h) inhibits the migration and invasion abilities of LN229 and U251MG glioma cells in a dose-dependent manner[1].
TMLZ-G46 (1-5 μM; 24 h) induces G0/G1 cell cycle arrest and apoptosis in LN229 and U251MG glioma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LN229 glioma cell line, U251MG glioma cell line, HS683 glioma cell line, U87MG glioma cell line, U118MG glioma cell line, U138MG glioma cell line, T98G glioma cell line
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Concentration:/
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Incubation Time:72 h
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Result:Showed potent antiproliferative activity, with half-maximal inhibitory concentration (IC50) values of 0.93 μM (LN229), 1.33 μM (U251MG), 2.07 μM (HS683), 2.05 μM (T98G), 4.82 μM (U87MG), 5.58 μM (U118MG), and 7.73 μM (U138MG).
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Cell Line:LN229 glioma cell line, U251MG glioma cell line
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Concentration:0.5, 1, 2, 4 μM
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Incubation Time:24 h
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Result:Downregulated SOX2 protein expression in a dose-dependent manner in both cell lines, with significant reduction observed at 2 μM and 4 μM.
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Cell Line:LN229 glioma cell line, U251MG glioma cell line
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Concentration:1, 5 μM
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Incubation Time:24 h
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Result:Induced G0/G1 cell cycle arrest.
Increased the G0/G1 fraction from 37.2% to 48.7% in LN229 cells at 5 μM.
Increased the G0/G1 fraction from 44.8% to 51.4% in U251MG cells at 5 μM.
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Cell Line:LN229 glioma cell line, U251MG glioma cell line
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Concentration:1, 5 μM
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Incubation Time:24 h
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Result:Induced apoptosis.
Reached apoptotic rates of 52.3% in LN229 cells at 5 μM.
Reached apoptotic rates of 12.5% in U251MG cells at 5 μM.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | MRT | F | CL |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5 (male) mg/kg | i.v. | 0.31 h | 0.083 h | 2290.90 ng/mL | 2546.66 ng·h/mL | 0.44 h | / | 76.67 mL/min |
| Rat[1] | 30 (male) mg/kg | p.o. | 11.90 h | 5.17 h | 592.79 ng/mL | 10405.67 ng·h/mL | 19.52 h | 68.1 % | / |
| Rat[1] | 5 (female) mg/kg | i.v. | 0.28 h | 0.083 h | 1772.01 ng/mL | 2006.24 ng·h/mL | 0.41 h | / | 130 mL/min |
| Rat[1] | 30 (female) mg/kg | p.o. | 14.7 h | 3.24 h | 327.53 ng/mL | 6340.88 ng·h/mL | 22.24 h | 52.7 % | / |
In Vivo
TMLZ-G46 (30 mg/kg; i.g.; once daily; 60 days) reduces tumor burden of orthotopic U251MG glioblastoma xenografts in mice and significantly prolongs their survival, with efficacy comparable to that of Temozolomide (HY-17364)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 6-8 weeks old, subcutaneous U251MG glioblastoma xenograft model)[1]
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Dosage:60 mg/kg
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Administration:p.o.; once daily; 28 days
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Result:Achieved a tumor growth inhibition rate of 83.7% compared to vehicle control.
Reduced mean tumor volume and tumor weight.
Showed no significant changes in body weight, organ index (heart, liver, spleen, lung, kidney), serum AST/ALT activities, or histopathological alterations of major organs.
Reduced PCNA- and Ki67-positive tumor cells significantly.
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Cell migration
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Colony Formation (Clonogenic) Assay
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- PCNA Immunodetection Proliferation Assay
- Flow cytometric DNA-content cell-cycle staining
- Protocol for Cell Counting and Cell Density Analysis
- Apoptosis Solutions
- Cell invasion
- Soft Agar Colony Formation Assay
- MTT Cell Proliferation Assay
Chemical Information
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CAS No. 3116767-83-7
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Appearance Solid
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Molecular Weight 575.74
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Formula C37H41N3O3
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Color White to off-white
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SMILES
O=C(/C(C#N)=C1C2=CC=CC=C2OC3=CC=CC=C3\1)NCCC4CCN(CC4)CC5=CC=C(C=C5)OCC6CCCCC6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 10 mg/mL (17.37 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, 6 months; -20°C, 1 month. 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. 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: ≥ 1 mg/mL (1.74 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (1.74 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
Purity & Documentation
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Data Sheet (277 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. 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 | 1.7369 mL | 8.6845 mL | 17.3690 mL | 43.4224 mL |
| 5 mM | 0.3474 mL | 1.7369 mL | 3.4738 mL | 8.6845 mL | |
| 10 mM | 0.1737 mL | 0.8684 mL | 1.7369 mL | 4.3422 mL | |
| 15 mM | 0.1158 mL | 0.5790 mL | 1.1579 mL | 2.8948 mL |
TMLZ-G46 Related Classifications
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