PLK1-IN-6
PLK1-IN-6 is a potent and selective PLK1 inhibitor, with an IC50 of 0.45 nM. PLK1-IN-6 shows significant anti-proliferative activities against cancer cells.
For research use only. We do not sell to patients.
- CAS No.: 3038489-04-9
- Formula: C28H37N9O3
- Molecular Weight:547.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
PLK1 0.45 nM (IC50) |
PLK2 5.73 nM (IC50) |
PLK3 7.56 nM (IC50) |
BRD4 156.3 nM (IC50) |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
26 nM
Compound: 21g
|
Antiproliferative activity against human HCT-116 cells incubated for 72 to 96 hrs by microplate reader analysis
Antiproliferative activity against human HCT-116 cells incubated for 72 to 96 hrs by microplate reader analysis
|
[PMID: 36889251] |
| MCF7 | IC50 |
8.64 nM
Compound: 21g
|
Antiproliferative activity against human MCF7 cells incubated for 72 to 96 hrs by microplate reader analysis
Antiproliferative activity against human MCF7 cells incubated for 72 to 96 hrs by microplate reader analysis
|
[PMID: 36889251] |
| MDA-MB-231 | IC50 |
14.8 nM
Compound: 21g
|
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 to 96 hrs by microplate reader analysis
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 to 96 hrs by microplate reader analysis
|
[PMID: 36889251] |
| MV4-11 | IC50 |
47.4 nM
Compound: 21g
|
Antiproliferative activity against human MV4-11 cells incubated for 72 to 96 hrs by microplate reader analysis
Antiproliferative activity against human MV4-11 cells incubated for 72 to 96 hrs by microplate reader analysis
|
[PMID: 36889251] |
PLK1-IN-6 (compound 21 g) shows significant anti-proliferative activities against four tumor-derived cell lines (MCF-7 IC50=8.64 nM, HCT-116 IC50=26.0 nM, MDA-MB-231 IC50=14.8 nM and MV4-11 IC50=47.4 nM)[1].
PLK1-IN-6 shows moderate metabolism and the half-life in human liver microsome is 25.7 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PLK1-IN-6 (10 mg/kg; i.g.) exhibits low clearance values and high plasma exposure (26800 ng•h/mL), with favorable bioavailability (11.4%) in Sprague Dawley rats[1].
PLK1-IN-6 (10 mg/kg; i.g.) exhibits long half-life (2.73 h), high plasma exposure (11227 ng•h/mL) and excellent bioavailability (77.4%) in Balb/c mice[1].
PLK1-IN-6 (20 mg/kg; i.g.) shows no apparent toxicity in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3038489-04-9
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Molecular Weight 547.65
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Formula C28H37N9O3
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SMILES
CC[C@@H]1C(N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C5=NOC(CN6CCNCC6)=N5)OC)C)=O
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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)