DHW-208
PI3K-IN-4 is a potent Pan-PI3K inhibitor. PI3K-IN-4 has high activity for three PI3K isoforms with the IC50 values of picomole. PI3K-IN-4 shows superior inhibitory activity against PI3Kα (IC50 = 0.20 nM), PI3Kβ (IC50 = 2.99 nM), PI3Kδ (IC50 = 0.48 nM) and PI3Kγ (IC50 = 0.58 nM) and has no significant activity against EGFR. PI3K-IN-4 inhibits cancer cell growth though PI3K/Akt signaling pathway, leading to the inhibition of colony formation and the induction of apoptosis. PI3K-IN-4 can be used for lung, colon and breast cancer research.
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- No. CAS: 2269470-35-9
- Fòrmula: C25H21F2N7O4S
- Peso molecular:553.54
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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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PI3Kα 0.20 nM (IC50) |
PI3Kβ 2.99 nM (IC50) |
PI3Kγ 0.58 nM (IC50) |
PI3Kδ 0.48 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
3.1 μM
Compound: 7b
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Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
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[PMID: 31097403] |
| HCT-116 | IC50 |
0.33 μM
Compound: 7b
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Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
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[PMID: 31097403] |
| HUVEC | IC50 |
19.6 μM
Compound: 7b
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Cytotoxicity against HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Cytotoxicity against HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
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[PMID: 31097403] |
| L02 | IC50 |
60 μM
Compound: 7b
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Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
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[PMID: 31097403] |
| MCF7 | IC50 |
0.22 μM
Compound: 7b
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Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay
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[PMID: 31097403] |
PI3K-IN-4 (compound 7b) (72h) shows antiproliferation activity against typically human cancer cells with IC50 values of 3.10 μM (A549), 0.33 μM (HCT116), and 0.22 μM (MCF-7), and displays much lower cytotoxicity in HUVEC (IC50 = 19.6 μM) and HL7702 normal cells (IC50 = 60.0 μM)[1].
PI3K-IN-4 (0.1-10 μM) decreases the phospho-Akt (S473) in a dose-dependent manner and down-regulated p-Akt/Akt ratio in MCF-7 cells, suggesting it might inhibit MCF-7 cell growth though PI3K/Akt signaling pathway[1].
PI3K-IN-4 (0.2-0.8 μM, 72 h) inhibits colony formation and inhibit the proliferation of MCF-7 cells in a dose-dependent manner[1].
PI3K-IN-4 (0.2-0.8 μM, 48 h) induces apoptosis in MCF-7 cells with markable nuclear fragmentation and condensation of chromatin[1].
PI3K-IN-4 forms four key hydrogen bonds with PI3K, one more than Omipalisib (HY-10297), which may contribute to its superior binding stability and activity[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 cells
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Concentration:0.2, 0.4 and 0.8 μM
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Incubation Time:72 h
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Result:Inhibited the cell proliferation in a dose-dependent manner.
Significantly inhibit colony formation at a concentration of 0.8 μM.
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Cell Line:MCF-7 cells
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Concentration:0.2, 0.4 and 0.8 μM
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Incubation Time:48 h
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Result:Induced cell apoptosis with the highest apoptosis percentage of 27.5 % at 0.8 μM.
Resulted in nuclear fragmentation and condensation of chromatin.
Chemical Information
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No. CAS 2269470-35-9
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Peso molecular 553.54
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Fòrmula C25H21F2N7O4S
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SMILES
COC(N=C1)=C(NS(=O)(C2=CC=C(F)C=C2F)=O)C=C1C3=CC=C(N=CN=C4NC5=CN(CCO)N=C5)C4=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)
DHW-208 Related Classifications
HY-128633 Related Classifications
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