PLK1-IN-10
Based on 1 publication(s) in Google Scholar
PLK1-IN-10 (Compound 4Bb) is an orally active PLK1 PBD (polo-box domain) inhibitor. PLK1-IN-10 blocks the interaction of PLK1 with the cell division regulator protein 1 (PRC1) and decreases the protein expression of the CDK1-Cyclin B1 complex. PLK1-IN-10 reacts with glutathione (GSH) to increase cellular oxidative stress, ultimately leading to cell death.
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- CAS No.: 2991469-21-5
- Formule: C23H22FN3O4S
- Masse moléculaire:455.50
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) PLK1-IN-10
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In Vivo Efficacy Study
Activité biologique
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PLK1 PBD |
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
10.56 μM
Compound: 4Bb
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Anticancer activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
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[PMID: 38657480] |
| A549/CDDP | IC50 |
2.65 μM
Compound: 4Bb
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Anticancer activity against human A549/DDP cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human A549/DDP cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
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[PMID: 38657480] |
| MCF7 | IC50 |
6.54 μM
Compound: 4Bb
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Anticancer activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
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[PMID: 38657480] |
| MGC-803 | IC50 |
3.2 μM
Compound: 4Bb
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Anticancer activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
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[PMID: 38657480] |
| NCI-H460 | IC50 |
2.31 μM
Compound: 4Bb
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Anticancer activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
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[PMID: 38657480] |
| SK-OV-3 | IC50 |
2.84 μM
Compound: 4Bb
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Anticancer activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
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[PMID: 38657480] |
| T-24 | IC50 |
2.9 μM
Compound: 4Bb
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Anticancer activity against human T24 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human T24 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
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[PMID: 38657480] |
PLK1-IN-10 (0-6 μM; 48 h) induces cell cycle arrest in the G2/M phase in A549 and A549/DDP cells, inhibiting cell proliferation[1].
PLK1-IN-10 (20 μM) stabilizes PLK1 protein in A549/DDP cells across a range of temperatures[1].
PLK1-IN-10 (5 μM; 24 h) reacts with GSH, producing a dose- and time-dependent fluorescent response, with higher fluorescence intensity in A549/DDP cells[1].
PLK1-IN-10 (0-9 μM; 48 h) increases intracellular ROS levels in A549/DDP cells[1].
PLK1-IN-10 (10 μM; 48 h) inhibits the interaction between PLK1 and PRC1, leading to the appearance of multinucleated cells[1].
PLK1-IN-10 shows an anticancer activity of IC50=7.83 μM against NCI-H1975 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, A549/DDP
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Concentration:0, 1.5, 3, 6 μM
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Incubation Time:48 h
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Result:Downregulated the expression of PLK1, CDK1, Cyclin B1, as well as significantly downregulated the expression of the CDK1-Cyclin B1 complex and Cdc25 protein.
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Cell Line:A549, A549/DDP
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Concentration:0, 1.5, 3, 6 μM
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Incubation Time:48 h
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Result:Significantly increased the number of A549 and A549/DDP cells in the G2/M phase, inducing mitotic catastrophe.
PLK1-IN-10 (30 mg/kg; p.o.; every two days for 20 days) effectively inhibits tumor growth in NCI-H1975 drug-resistant xenograft mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A549/DDP drug-resistant xenograft mice[1]
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Dosage:30, 50 mg/kg
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Administration:i.p.; once every two days for 32 days
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Result:TGI reached 42% for the 30 mg/kg group and 62% for the 50 mg/kg group.
Extended the median survival time from 38 days in the control group to 53 days in the 30 mg/kg group and 62 days in the 50 mg/kg group.
Had no significant impact on the body weight and major organs of the mice, except for a slight difference in heart index observed in the 30 mg/kg group.
Significantly reduced the number of Ki-67 positive cells in the tumor tissue.
Showed no significant differences in H&E staining of major organs, further confirming its good biosafety.
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Animal Model:NCI-H1975 drug-resistant xenograft mice[1]
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Dosage:30 mg/kg
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Administration:p.o.; once every two days for 20 days
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Result:TGI reached 44%. Caused no harm to the body weight and major organs of the mice.
Chemical Information
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CAS No. 2991469-21-5
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Masse moléculaire 455.50
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Formule C23H22FN3O4S
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SMILES
CN(C)CCN(C1=O)C(C2=CC=C(S(NCC3=CC=C(F)C=C3)(=O)=O)C4=CC=CC1=C42)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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J Exp Clin Cancer Res
CCNY-mediated phosphorylation and TET2-BACH1-driven DNA demethylation activate PRC1 to augment NSCLC progression. [Abstract]2025 Jul 15;44(1):206. PMID: 40665337
PLK1-IN-10 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 15;44(1):206. [Abstract]
H1299 cells were subcutaneously injected into nude mice to construct xenografts, followed by intratumoral injections (10 mg/kg; Bobcat339, HPPE, or PLK1-IN-10) starting from day 7. Volume of xenograft tumors by week.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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