MN33-47
MN33-47 is a multi-target anti-tumor compound with broad-spectrum anti-proliferative activity. MN33-47 relieves the inhibition of the mitochondrial apoptosis pathway by downregulating the anti-apoptotic protein Bcl-2, while activating caspase-3 and inhibiting Topoisomerase I activity, thereby promoting its degradation through the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-47 can also induce DNA cross-linking and G2/M cell cycle arrest, inhibit cancer cell migration and activate the mitochondrial apoptosis pathway, thus exerting potent anti-tumor effects. MN33-47 can improve the water solubility of SN-38 (HY-13704), and exhibits dose-dependent tumor growth inhibition effects in CT26 tumor-bearing mouse models without obvious toxic and side effects. MN33-47 can be used in related studies on colorectal adenocarcinoma, cervical adenocarcinoma, hepatocellular carcinoma, alveolar basal epithelial adenocarcinoma, gastric cancer and colon cancer.
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- Formel: C27H28Cl3N3O6
- Molecular Weight:596.89
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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Topoisomerase I |
Caspase 3 |
Bcl-2 |
MN33-47 (0.038-100000 nM; 72 h) potently inhibits the proliferation of HCT-15, HeLa, HepG2, A549, HGC-27, and CT26 cells with IC50=4.77-252.10 nM, showing enhanced activity against HeLa, HepG2, and CT26 cells relative to control treatments[1].
MN33-47 (100 nM; 24, 48 h) significantly inhibits the migration of CT26 cells at 24 h and 48 h, showing greater efficacy than single-agent chlormethine hydrochloride (HY-B1253) (CH) or SN-38 (HY-13704)[1].
MN33-47 (100 nM; 48 h) induces G2/M phase arrest in 46.3% of CT26 cells after 48 h, showing stronger cell cycle blockade than CH, SN-38, or their physical mixture[1].
MN33-47 (100 nM; 48 h) induces apoptosis in 50.63% of CT26 cells after 48 h, exhibiting significantly greater pro-apoptotic efficacy than CH, SN-38, or their physical mixture[1].
MN33-47 (1-10000 nM, 1 μM; 72 h) dose-dependently reduces Topo I protein levels in CT26 cells via the ubiquitin-proteasome and autophagy-lysosome pathways, and at 1 μM, it more effectively downregulates Bcl-2 and activates caspase-3 than SN-38, CH, or their physical mixture[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-15, HeLa, HepG2, A549, HGC-27, CT26
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Concentration:0.038-100000 nM
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Incubation Time:72 h
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Result:Exhibited broad-spectrum antiproliferative activity across all six cell lines, with IC50 values of 8.06 nM (HCT-15), 24.43 nM (HeLa), 6.24 nM (HepG2), 252.10 nM (A549), 34.55 nM (HGC-27), and 4.77 nM (CT26).
Showed superior potency to control groups including SN-38, CH, and their physical mixture in select cell lines, with significantly enhanced inhibition against HeLa, HepG2, and CT26 cells compared to MN33-45.
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Cell Line:CT26
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Concentration:100 nM
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Incubation Time:48 h
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Result:Induced substantial G2/M phase arrest in CT26 cells, with 46.3% of cells in the G2/M phase, compared to 8.98% in the untreated control group.
Showed a significantly stronger arrest than that induced by CH, SN-38, or their physical mixture.
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Cell Line:CT26
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Concentration:100 nM
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Incubation Time:48 h
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Result:Induced an apoptosis rate of 50.63% in CT26 cells, which was significantly higher than the rates induced by CH (15.91%), SN-38 (25.00%), or their physical mixture (38.20%).
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Cell Line:CT26
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Concentration:1-10000 nM (72 h incubation); 1 μM (72 h incubation)
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Incubation Time:72 h
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Result:Reduced Topo I protein levels in a dose-dependent manner, with the strongest inhibition observed at 10 μM.
At 1 μM, inhibited Topo I expression more effectively than SN-38, CH, or their physical mixture.
Downregulated Bcl-2 expression and reduced total caspase-3 protein levels (indicating activation of caspase-3) more strongly than control groups at 1 μM.
The reduction in Topo I levels induced by MN33-47 was reversed by the proteasome inhibitor MG132 and autophagy-lysosome inhibitor chloroquine.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice with Colon cancer (female, 4-5 weeks old, 19-21 g, subcutaneous colon cancer xenograft)[1]
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Dosage:1.56 mg/kg; 3.12 mg/kg; 6.24 mg/kg
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Administration:i.p.; daily; 10 days
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Result:Achieved a tumor inhibition rate of 75.73% in the 6.24 mg/kg group.
Showed dose-dependent tumor growth inhibition.
Reduced tumor volume markedly in all dose groups compared to vehicle control, with the high-dose group having the smallest tumor mass.
Induced dose-dependent increases in tumor necrotic areas, reduced tumor cell density, and nuclear condensation, with the high-dose group showing the most pronounced effects.
Caused no significant body weight loss in any dose group.
Maintained serum ALT, AST, BUN, and CREA levels within normal reference ranges in all dose groups.
Showed no significant pathological alterations in heart, liver, spleen, lung, and kidney tissues in any dose group.
Chemical Information
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Molecular Weight 596.89
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Formel C27H28Cl3N3O6
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SMILES
CCC1=C2C(C(N3C2)=CC([C@@](O)(CC)C(OC4)=O)=C4C3=O)=NC5=CC=C(OC(N(CCCl)CCCl)=O)C=C51.Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
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Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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