MNK1/2-IN-11
MNK1/2-IN-11 is a potent, selective and orally active MNK1/2 inhibitor with MNK1 IC50 of 1.2 nM, MNK2 IC50 of 1.3 nM. MNK1/2-IN-11 reduces eukaryotic translation initiation factor 4E phosphorylation, decreases Mcl-1 and Cyclin D1 expression. MNK1/2-IN-11 inhibits tumor growth in mouse CT26 colorectal tumor models. MNK1/2-IN-11 can be used for the research of colorectal cancer.
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- Fòrmula: C30H31N7O3
- Peso molecular:537.61
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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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Actividad biológica
Descripciòn
IC50 & Target
[1]|
MNK1 1.2 nM (IC50) |
MNK2 1.3 nM (IC50) |
Mcl-1 |
In Vitro
MNK1/2-IN-11 (compound 34) (72 h) inhibits the proliferation of CT26, HCT116, A549, MDA-MB-231, and LNCaP solid tumor cell lines with IC50 valuesof 11.7, 18.8, 13.0, 26.6 and 19.6 μM[1].
MNK1/2-IN-11 (1.25-5 μM; 3 days) dose-dependently inhibits eIF4E phosphorylation and reduces Mcl-1 and Cyclin D1 expression in CT26 colorectal cancer cells without affecting total eIF4E, MNK1, or Bcl-2 levels[1].
MNK1/2-IN-11 (1 μM) exhibits high kinase selectivity, with significant inhibition limited primarily to MNK1 and MNK2 at 1 μM, and only moderate inhibition of PIM1/3, JNK1/2/3, NEK1, and MET[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CT26
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Concentration:1.25; 2.5; 5; 10 μM
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Incubation Time:3 days
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Result:Dose-dependently inhibited phosphorylation of eIF4E at Ser209.
Suppressed the expression of downstream oncoproteins Mcl-1 and Cyclin D1.
Did not alter total eIF4E, MNK1, or Bcl-2 protein levels.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Balb/c mice (5-6 weeks old) subcutaneously injected with CT26 cells[1]
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Dosage:50 mg/kg
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Administration:p.o.; every other day; 14 days
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Result:Achieved 36% tumor growth inhibition (TGI).
Combined with anti-mPD-1 antibody achieved 76% TGI.
Markedly augmented CD8+ T cell infiltration compared to monotherapy.
Caused no significant body weight loss.
Chemical Information
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Peso molecular 537.61
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Fòrmula C30H31N7O3
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SMILES
O=C(C1=CC=C(C2=NN3C(C=C2)=NC=C3C(O4)=CC5=C4C=CN=C5N6C[C@H](N(C)C)CC6)C=C1)N7CCOCC7
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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)
MNK1/2-IN-11 Related Classifications
HY-183328 Related Classifications
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