TMLZ-G46
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.
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- No. CAS: 3116767-83-7
- Fòrmula: C37H41N3O3
- Peso molecular:575.74
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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.
| 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 % | / |
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.
Chemical Information
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No. CAS 3116767-83-7
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Peso molecular 575.74
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Fòrmula C37H41N3O3
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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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TMLZ-G46 Related Classifications
HY-182358 Related Classifications
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