FKA-9i
FKA-9i is an orally active anticancer agent. FKA-9i directly binds to and promotes the degradation of oncoproteins LRPPRC (kd: 7.387 μM), YBX1 (kd: 16.52 μM) and RPN1 (kd: 26.82 μM). FKA-9i inhibits the MAPK signaling pathway and mitochondrial oxidative phosphorylation. FKA-9i also induces cancer cell cycle arrest, apoptosis, mitochondrial dysfunction and ROS accumulation. FKA-9i can be used in the research of tumors such as gastric cancer.
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- CAS No.: 3060515-85-4
- Formule: C30H26F2N2O9S2
- Masse moléculaire:660.66
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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CDK1 |
Caspase 3 |
Bcl-2 |
FKA-9i (0-72 h) inhibits the proliferation of HGC27, KYSE70, KYSE450, HCT116 and A549 cancer cells, with IC50 values of 1.49, 3.15, 2.25, 3.53 and 4.48 μM, respectively[1].
FKA-9i (0-8 μM; 0-48 h) inhibits tumor cell proliferation, and induces cell cycle arrest and apoptosis[1].
FKA-9i (0-8 μM; 0-48 h) reduces the stability of LRPPRC, YBX1 and RPN1 proteins in HGC27 cells and promotes their degradation[1].
FKA-9i (48 h) inhibits the expression of genes related to the MAPK signaling pathway and suppresses the MAPK cascade in HGC27 cells[1].
FKA-9i (4-8 μM; 48 h) dose-dependently increases intracellular ROS levels in HGC27 and HCT116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HGC27, KYSE450, HCT116
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Concentration:0, 2, 4 and 8 μM
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Incubation Time:48 h
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Result:Induced G1 phase arrest in HGC27 and HCT116 cells, and S phase arrest in KYSE450 cells.
Downregulated cell cycle regulators CCND1 and CDK1.
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Cell Line:HGC27, KYSE450, HCT116
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Concentration:0, 2, 4 and 8 μM
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Incubation Time:48 h
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Result:Reduced protein expression levels of caspase-3 and anti-apoptotic protein Bcl-2.
FKA-9i (100-200 mg/kg; oral gavage; 10 days) shows no obvious acute organ toxicity in C57BL/6 mice[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-nu nude mice (female, 6-week-old) treated HGC27 cells[1]
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Dosage:2.5 mg/kg/day; 5 mg/kg/day
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Administration:Oral gavage; 31 days
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Result:Reduced mean tumor volume, tumor number, and tumor weight.
Showed no significant differences in body weight compared to the control group.
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Animal Model:C57BL/6 mice (male, 8-week-old)[1]
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Dosage:100 mg/kg/day; 200 mg/kg/day
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Administration:Oral gavage; 10 days
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Result:Showed no significant differences in body weight organ weights compared to the control group.
Observed no histopathological changes (H&E staining of liver and kidney tissues) compared to the control group.
Chemical Information
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CAS No. 3060515-85-4
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Masse moléculaire 660.66
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Formule C30H26F2N2O9S2
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SMILES
COC1=CC(OC)=C(C(CC(C2=CC(S(NC3=CC=C(F)C=C3)(=O)=O)=C(OC)C=C2)O4)=O)C4=C1S(NC5=CC=C(F)C=C5)(=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FKA-9i Related Classifications
HY-181098 Related Classifications
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