MG16
MG16 is a prodrug of 10-Methoxycamptothecin (HY-N0446). MG16 downregulates CDK6 and upregulates ASK1. MG16 induces cell cycle arrest and Apoptosis. MG16 exhibits anticancer activity against Lewis lung carcinoma, small cell lung cancer, and non-small cell lung cancer.
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- No. CAS: 2349329-01-5
- Fòrmula: C23H22ClN3O6
- Peso molecular:471.89
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Actividad biológica
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Actividad biológica
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CDK6 |
MG16 (48 h) potently inhibits the proliferation of LLC, A549 and H446 lung cancer cells in vitro, with IC50 values of 408.2 ± 32.4, 613.1 ± 54.7 and 140.4 ± 10.4 nM[1], respectively.
Treatment with MG16 (0.1-100 nM; 48 h) induces dose-dependent apoptosis in A549 and H446 lung cancer cells, and its pro-apoptotic activity in both cell lines is significantly stronger than that of SN-38[1].
MG16 (90.1-1 μM for A549, 10-100 nM for H446; 24 h) regulates the expression of key apoptotic proteins and induces robust Caspase-3 activation in A549 and H446 lung cancer cells after 24 h of treatment, with a more prominent Caspase-3 activation effect than SN-38[1].
MG16 (613.1 nM; 48 h) induces cell cycle arrest at the G0/G1 phase in A549 lung cancer cells following 48 h of treatment at its IC50 concentration[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 lung cancer cells, H446 lung cancer cells
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Concentration:0.1-1 μM (A549 cells); 10-100 nM (H446 cells)
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Incubation Time:24 h
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Result:Upregulated the proapoptotic protein Bax, downregulated the antiapoptotic protein Bcl-2, and strongly activated caspase-3 in A549 cells, with significantly higher cleaved caspase-3 levels than SN-38 at both tested concentrations.
Upregulated Bax, downregulated Bcl-2, and activated caspase-3 in H446 cells, with significantly higher cleaved caspase-3 levels than SN-38 at both tested concentrations, especially at 100 nM.
MG16 (5 mg/kg; i.v.; every other day) achieves an 80.5% tumor inhibition rate, showing potent lung cancer growth suppression in a mouse A549 subcutaneous tumor model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 2349329-01-5
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Peso molecular 471.89
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Fòrmula C23H22ClN3O6
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SMILES
CC[C@]1(C(OCC2=C1C=C3C4=NC5=CC=C(C=C5C=C4CN3C2=O)OC)=O)OC(CN)=O.Cl
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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)
MG16 Related Classifications
HY-182071 Related Classifications
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- MG16
- 2349329-01-5
- MG 16
- MG-16
- Drug Derivative
- Apoptosis
- CDK
- ASK1
- human lung cancer xenograft mouse models
- Lewis lung carcinoma cells
- mitochondrial apoptotic pathways
- lung cancer cells
- human lung cancer cell lines
- G0/G1 cell cycle arrest
- cyclin-dependent kinase 6
- G1-to-S phase cell cycle transition
- syngeneic Lewis lung carcinoma mouse models
- apoptosis signal-regulating kinase 1
- Inhibitor
- inhibitor
- inhibit