Hit20
Hit20 is a PI3Kα selective inhibitor, inhibits PI3Kα kinase activity, suppresses PI3Kα phosphorylation. Hit20 suppresses proliferation, colony formation, migration, and invasion of colon cancer cells. Hit20 can be used for the research of colon cancer.
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- No. CAS: 536714-52-0
- Fòrmula: C22H17ClN6O2S2
- Peso molecular:496.99
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
Hit20 (10 μM) inhibits PI3Kα kinase activity in a cell-free assay with 40.24% inhibition at 10 μM[1].
Hit20 (0-100 μM; 48 h) inhibits proliferation of HCT-116, MCF-7, A549, and H1299 cells with the highest potency against HCT-116 cells (IC50 7.26 μM)[1].
Hit20 (1, 3, 6 μM; 48 h treatment, 14 days culture) reduces colony formation of HCT-116 cells in a concentration-dependent manner[1].
Hit20 (1, 3, 6 μM; 48 h) inhibits wound healing of HCT-116 cells in concentration- and time-dependent manners[1].
Hit20 (1, 3, 6 μM; 48 h) inhibits migration and invasion of HCT-116 cells in a concentration-dependent manner[1].
Hit20 (3, 6, 9 μM; 48 h) induces apoptosis of HCT-116 cells in a concentration-dependent manner[1].
Hit20 (3, 6, 9 μM; 48 h) modulates expression of apoptosis-related proteins (Caspase-3/9, cleaved Caspase-3/9, Bcl-2, Bax) in HCT-116 cells in a concentration-dependent manner[1].
Hit20 (3, 6, 9 μM; 48 h) inhibits phosphorylation of PI3Kα and Akt in HCT-116 cells in a concentration-dependent manner, suppressing the PI3K/Akt signaling pathway[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7, HCT-116, A549, H1299 cells
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Concentration:7.26 μM (IC50, HCT-116); 27.37 μM (IC50, MCF-7); 13.40 μM (IC50, A549); 12.22 μM (IC50, H1299)
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Incubation Time:48 h
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Result:Exhibited the highest anti-proliferative activity against HCT-116 cells with an IC50 of 7.26 μM, while showing weaker activity against MCF-7 (IC50 27.37 μM), A549 (IC50 13.40 μM), and H1299 (IC50 12.22 μM) cells.
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Cell Line:HCT-116 cells
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Concentration:1, 3, 6 μM
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Incubation Time:48 h (treatment); 14 days (culture)
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Result:Reduced colony formation in a concentration-dependent manner; showed lower colony numbers in Hit20-treated groups compared to the control.
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Cell Line:HCT-116 cells
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Concentration:1, 3, 6 μM
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Incubation Time:48 h
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Result:Decreased wound healing rates in a concentration- and time-dependent manner; reached 33.66% (1 μM), 26.61% (3 μM), and 24.90% (6 μM) at 48 h compared to the control.
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Cell Line:HCT-116 cells
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Concentration:3, 6, 9 μM
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Incubation Time:48 h
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Result:Increased total apoptosis rates in a concentration-dependent manner; reached 7.14% (3 μM), 10.51% (6 μM), and 17.89% (9 μM) compared to the control’s 5.86%.
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Cell Line:HCT-116 cells
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Concentration:3, 6, 9 μM
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Incubation Time:48 h
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Result:Downregulated expression of Caspase-3/9 and Bcl-2, while upregulated cleaved Caspase-3/9 and Bax in a concentration-dependent manner.\nReduced phosphorylation levels of PI3Kα (p85α) and Akt (Ser473) in a concentration-dependent manner, decreased p-PI3K/PI3K and p-Akt/Akt ratios.
Chemical Information
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No. CAS 536714-52-0
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Peso molecular 496.99
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Fòrmula C22H17ClN6O2S2
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SMILES
CCC1=NN=C(S1)NC(CSC2=NC3=C(C(N2C4=CC=C(C=C4)Cl)=O)NC5=CC=CC=C53)=O
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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)
Hit20 Related Classifications
HY-181150 Related Classifications
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