HSND80
HSND80 (Compound 1) is an orally active inhibitor of MNK/p70S6K, with Kd values of 44 nM against MNK1 and 4 nM against MNK2. HSND80 has a longer target residence time of 45 mins and 58 mins against MNK1 and MNK2 respectively. HSND80 can suppress non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppress Triple-Negative Breast Cancer (TNBC) in vitro.
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- Fòrmula: C33H35F3N8O2
- Peso molecular:632.68
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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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MNK1 44 nM (Kd) |
MNK2 4 nM (Kd) |
p70S6K |
HSND80 (0.1-104nM, 72 h) inhibits cells growth of MDA-MB-23, MDA-MB-468, 4T1, T47D, MCF-7, HOP-92, NCI-H226, NCI-H522, EKVX, NCI-H322M, A549, NCI-H23, NCI-H460, HOP-62, KLN205 with IC50 values of 8.8 nM, 18.3 nM, 0.93 nM, 84.2 nM, 18.5 nM, 27 nM, 29.5 nM, 31.6 nM, 38 nM, 57.5 nM, 79.4 nM, 107.2 nM, 107.2 nM, 144.5 nM, 360 nM, respectively[1].
HSND80 (200 nM, 30 h) induces G1 arrest[1].
HSND80 (0.5-3 μM, 4 h) downregulates phosphorylation levels of eIF4E (MNK1/2 target), along with S6 and eIF4B (p70S6K targets)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-23, MDA-MB-468, 4T1, T47D, MCF-7, HOP-92, NCI-H226, NCI-H522, EKVX, NCI-H322M, A549, NCI-H23, NCI-H460, HOP-62, KLN205
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Concentration:0.1-104 nM
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Incubation Time:72 h
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Result:Reduced cell viability.
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Cell Line:MDA-MB-231
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Concentration:200 nM
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Incubation Time:30 h
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Result:Induced G1 arrest.
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Cell Line:MDA-MB-231
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Concentration:0.5 μM, 1 μM, 3 μM
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Incubation Time:4 h
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Result:Downregulated phosphorylation levels of eIF4E (MNK1/2 target), along with S6 and eIF4B (p70S6K targets).
HSND80 (15 mg/kg, 30 mg/kg; p.o.; 5 days on, 2 days off, 15 days) leads to a reduction in tumor volumes in DBA/2 mice [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:DBA/2 mice (6-8 weeks) were subcutaneously injected with 0.7 x 106 KLN 205 cells per 100 μL, administrated after 6 months [1]
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Dosage:15 or 30 mg/kg
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Administration:Oral gavage (p.o.); 5 days on, 2 days off; total 15 days.
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Result:Led to a reduction in tumor volumes.
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Animal Model:Male CD1 mice[1]
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Dosage:10 mg/kg
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Administration:Oral gavage (p.o.) and blood sampling was done between 0.25-24 h.
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Result:Improved oral bioavailability, the maximum plasma concentration was 176 ng/mL at 2 h, which diminished to 2.5 ng/mL at 24 h.
Chemical Information
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Peso molecular 632.68
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Fòrmula C33H35F3N8O2
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SMILES
O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)C3=CN=CC(C#CC4=CN=C5C=CC(N6C[C@H](C)O[C@H](C)C6)=NN54)=C3
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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)
HSND80 Related Classifications
HY-172392 Related Classifications
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