MEK/PI3K-IN-2
MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines.
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- CAS. Nr.: 2281803-33-4
- Formel: C38H41F5IN9O7
- Molecular Weight:957.68
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
|
MEK1 352 ± 2 nM (IC50) |
PI3Kα 107 ± 21 nM (IC50) |
PI3Kδ 137 ± 7 nM (IC50) |
PI3Kγ 2567 ± 364 nM (IC50) |
PI3Kβ 3880 ± 725 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
8.5 μM
Compound: 6s
|
Antiproliferative activity against human A-375 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Fluor cell viability assay
Antiproliferative activity against human A-375 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Fluor cell viability assay
|
[PMID: 34802837] |
| D54 cell line | IC50 |
9.9 μM
Compound: 6s
|
Antiproliferative activity against human D54 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Fluor cell viability assay
Antiproliferative activity against human D54 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Fluor cell viability assay
|
[PMID: 34802837] |
| SET-2 | IC50 |
7 μM
Compound: 6s
|
Antiproliferative activity against human SET-2 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Fluor cell viability assay
Antiproliferative activity against human SET-2 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter-Fluor cell viability assay
|
[PMID: 34802837] |
Chemical Information
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CAS. Nr. 2281803-33-4
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Molecular Weight 957.68
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Formel C38H41F5IN9O7
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SMILES
O=C(C1=C(C(F)=C(C=C1)F)NC2=CC=C(C=C2F)I)NOCCOCCOCCOCCN(C3=NC(N4CCOCC4)=NC(N5C(C(F)F)=NC6=C5C=CC=C6)=N3)CCO
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)