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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3060515-85-4
- 分子式: C30H26F2N2O9S2
- 分子量:660.66
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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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.
化学情報
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CAS 番号 3060515-85-4
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分子量 660.66
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
FKA-9i 関連分類
HY-181098 関連分類
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