PLK1-IN-17
PLK1-IN-17 is a potent PLK1 inhibitor with an IC50 of 2 nM. PLK1-IN-17 shows high selectivity for PLK2 and CDK2/A, moderate selectivity for PLK3, only weak activity against CK2, FLT3 and NEK6, and no activity against PDGFR, ALK and another 37 kinases. PLK1-IN-17 inhibits the proliferation of ovarian cancer cells and can be used in ovarian cancer-related research.
For research use only. We do not sell to patients.
- CAS No.: 1034617-66-7
- Formula: C22H23F3N8O2
- Molecular Weight:488.47
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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
Biological Activity
Description
IC50 & Target
[1]|
PLK1 2 nM (IC50) |
FLT3 194 nM (IC50) |
CK2 59 nM (IC50) |
NEK6 595 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| A2780 | IC50 |
0.03 μM
Compound: 17
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Antiproliferative activity against human A2780 cells after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human A2780 cells after 72 hrs by CellTiter-Glo assay
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[PMID: 20932759] |
In Vitro
PLK1-IN-17 potently inhibits recombinant PLK1 with an IC50 of 0.002 μM, while showing high selectivity over PLK2, CDK2/A, and moderate selectivity over PLK3[1].
PLK1-IN-17 potently inhibits PLK1 with an IC50 of 0.002 μM, shows weak activity against CK2, FLT3, and NEK6, and is inactive against PDGFR, ALK, and 37 additional tested kinases[1].
PLK1-IN-17 inhibits A2780 ovarian carcinoma cell proliferation with an IC50 of 0.03 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1034617-66-7
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Molecular Weight 488.47
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Formula C22H23F3N8O2
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SMILES
O=C(C1=NN(C)C2=C1CCC3=C2N=C(NC4=CC(N5CCNCC5)=CC=C4OC(F)(F)F)N=C3)N
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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)
PLK1-IN-17 Related Classifications
HY-184863 Related Classifications
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