LNP23
LNP23 is a selective PI3Kα inhibitor with an IC50 of 5.15 nM. LNP23 inhibits PI3K/AKT signaling and induces apoptosis and G1 phase arrest in MCF-7 cells. LNP23 also inhibits cancer cell proliferation, colony formation, and migration. LNP23 can be used for breast cancer and lung adenocarcinoma research.
For research use only. We do not sell to patients.
- CAS No.: 3136664-01-9
- Formula: C30H32F2N8O4
- Molecular Weight:606.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
PI3Kα 5.15 nM (IC50) |
PI3Kβ 84.11 nM (IC50) |
PI3Kδ 19.82 nM (IC50) |
PI3Kγ 162.71 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | IC50 |
6.85 μM
|
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
|
PMC9268102 |
| MCF7 | IC50 |
1.29 μM
|
Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
|
PMC9268102 |
| H1975 | IC50 |
2.13 μM
|
Antiproliferative activity against human H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Antiproliferative activity against human H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
|
PMC9268102 |
| WI-38 | IC50 |
26.49 μM
|
Cytotoxicity against noncancerous human WI-38 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Cytotoxicity against noncancerous human WI-38 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
|
PMC9268102 |
In Vitro
LNP23 inhibits PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ with IC50 values of 5.15, 84.11, 19.82, and 162.71 nM, respectively[1].
LNP23 (72 h) inhibits the proliferation of MDA-MB-231, MCF-7, and H1975 cells with IC50 values of 6.85, 1.29, and 2.13 μM, respectively, and an IC50 of 26.49 μM against WI-38 cells[1].
LNP23 (0.5-4.5 μM; 72 h) decreases p-PI3K and p-AKT protein levels in a concentration-dependent manner in MCF-7 cells[1].
LNP23 (0.5-4.5 μM; 48 h) induces nuclear condensation and fragmentation in MCF-7 cells[1].
LNP23 (0.5-4.5 μM; 24 h) reduces the clonogenic ability of MCF-7 cells in a concentration-dependent manner[1].
LNP23 (0.5-4.5 μM; 48 h) inhibits MCF-7 cell migration in a concentration-dependent manner[1].
LNP23 (0.5-4.5 μM; 48 h) induces early and late apoptotic morphology in a concentration-dependent manner and reduces cell number in MCF-7 cells[1].
LNP23 (0.5-4.5 μM; 48 h) increases the apoptosis rate of MCF-7 cells in a concentration-dependent manner, with a total apoptosis rate of 36.35% at 4.5 μM, compared to 5.43% in the control group[1].
LNP23 (0.5-4.5 μM; 24 h) induces G1 phase arrest in MCF-7 cells in a concentration-dependent manner, with the proportion of G1 phase cells increasing from 54.05% in the control group to 60.62%, 68.8%, and 73.73%[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
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Concentration:0.5, 1.5, 4.5 μM
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Incubation Time:72 h
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Result:Significantly reduced the expression levels of p-PI3K and p-AKT proteins with increasing concentration.
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Cell Line:MCF-7
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Concentration:0.5, 1.5, 4.5 μM
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Incubation Time:48 h
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Result:Increased early yellow-green and late orange-red apoptotic morphology in a concentration-dependent manner.
Reduced cell number with increasing concentration.
Induced nuclear condensation and fragmentation.
Increased nuclear fluorescence intensity.
Increased total apoptotic cells in a concentration-dependent manner.
Increased total apoptosis to 36.35% at 4.5 μM compared with 5.43% in control cells.
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Cell Line:MCF-7
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Concentration:0.5, 1.5, 4.5 μM
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Incubation Time:24 h
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Result:Led to a progressive accumulation of cells in the G1 phase.
Increased the percentage of cells in G1 from 54.05% in the control group to 60.62% at 0.5 μM, 68.8% at 1.5 μM, and 73.73% at 4.5 μM.
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Cell Line:MCF-7
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Concentration:0.5, 1.5, 4.5 μM
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Incubation Time:24 h (then 14 days incubation)
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Result:A gradual decline in the number of cell clones was observed with increasing concentration.
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Cell Line:MCF-7
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Concentration:0.5, 1.5, 4.5 μM
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Incubation Time:48 h
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Result:The number of migrated cells gradually decreased with increasing concentration.
Chemical Information
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CAS No. 3136664-01-9
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Molecular Weight 606.62
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Formula C30H32F2N8O4
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SMILES
O=C(N1CCN(C2=NC(N3C(C(F)F)=NC4=CC=CC=C34)=NC(N5CCOCC5)=N2)CC1)/C=C/C6=CC=C(OC)C(OC)=C6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)