MEK/PI3K-IN-1
MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines.
For research use only. We do not sell to patients.
- CAS No.: 2281803-28-7
- Formula: C36H37F5IN9O6
- Molecular Weight:913.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All MEK Isoforms
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Biological Activity
Description
IC50 & Target
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MEK1 124 ± 11 nM (IC50) |
PI3Kα 130 ± 13 nM (IC50) |
PI3Kδ 236 ± 29 nM (IC50) |
PI3Kβ 1537 ± 188 nM (IC50) |
PI3Kγ 2745 ± 485 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
10.7 μM
Compound: 6r
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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
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[PMID: 34802837] |
| D54 cell line | IC50 |
17.3 μM
Compound: 6r
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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
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[PMID: 34802837] |
| SET-2 | IC50 |
10.7 μM
Compound: 6r
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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
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[PMID: 34802837] |
Chemical Information
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CAS No. 2281803-28-7
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Molecular Weight 913.63
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Formula C36H37F5IN9O6
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SMILES
O=C(C1=C(C(F)=C(C=C1)F)NC2=CC=C(C=C2F)I)NOCCOCCOCCOCCNC3=NC(N4CCOCC4)=NC(N5C(C(F)F)=NC6=C5C=CC=C6)=N3
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MEK/PI3K-IN-1 Related Classifications
HY-144692 Related Classifications
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