2. Cell Cycle/DNA Damage
  3. Polo-like Kinase (PLK)
  4. PLK1-IN-12

PLK1-IN-12 is a highly selective and orally active PLK1 inhibitor with an IC50 of 20 nM. PLK1-IN-12 shows more selective for PLK1 than PLK2 (IC50: >10000 nM) and PLK3 (IC50: 3953 nM). PLK1-IN-12 exhibits anticancer potency across a broad spectrum of cell lines. PLK1-IN-12 can be used in anti-leukemia research.

For research use only. We do not sell to patients.

PLK1-IN-12 Chemical Structure

PLK1-IN-12 Chemical Structure

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PLK1-IN-12 Related Antibodies

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Description

PLK1-IN-12 is a highly selective and orally active PLK1 inhibitor with an IC50 of 20 nM. PLK1-IN-12 shows more selective for PLK1 than PLK2 (IC50: >10000 nM) and PLK3 (IC50: 3953 nM). PLK1-IN-12 exhibits anticancer potency across a broad spectrum of cell lines. PLK1-IN-12 can be used in anti-leukemia research[1].

IC50 & Target[1]

PLK1

20 nM (IC50)

PLK2

>10000 nM (IC50)

PLK3

3953 nM (IC50)

In Vitro

PLK1-IN-12 (Compound B31) (0.508 nM-10 μM, 24 h) shows antiproliferative effects in H460 (IC50: 12 nM), A549 (IC50: 32 nM), SW620 (IC50: 8.2 nM), HL-60 (IC50: 59 nM), K562 (IC50: 0.08 nM) and CCRF-CEM (IC50: 41 nM) cell lines[1].
PLK1-IN-12 (1 μM, 5 min) shows rapid clearance in human, mouse and dog liver microsomes (Clint: 68.3-210 μL/min/mg protein)[1].
PLK1-IN-12 (0.1-30 μM, 24 h) has a low inhibitory effect on HEK293T cells viability (68%)[1].
PLK1-IN-12 (0.4-100 μM) has a low inhibitory effect on hERG potassium channels (IC50: 44.2 μM), indicating a low risk of cardiotoxicity[1].
PLK1-IN-12 (10 μM, 5-30 min) has no inhibitory effect on CYP1A2, CYP3A4, CYP2D6, CYP2B6 and CYP2C8, and only has weak inhibitory effects on CYP2C9 and CYP2C19, indicating that it is stable in both human and rat hepatocytes and has a low possibility of drug interactions[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PLK1-IN-12 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: H460、PC-9、A549、SW620、HL-60、K562、CCRF-CEM and KG-1 cell lines
Concentration: 1.00 × 10-5, 3.33 × 10-6, 1.11 × 10-6, 3.7 × 10-7, 1.23 × 10-7, 4.12 × 10-8, 1.37 × 10-8, 4.57 × 10-9, 1.52 × 10-9, and 5.08 × 10-10 mol/L
Incubation Time: 24 h
Result: Showed antiproliferative effects in H460 (IC50: 12 nM), A549 (IC50: 32 nM), SW620 (IC50: 8.2 nM), HL-60 (IC50: 59 nM), K562 (IC50: 0.08 nM) and CCRF-CEM (IC50: 41 nM) cell lines.

Cell Cytotoxicity Assay[1]

Cell Line: HEK293T cells
Concentration: 0.1, 0.3, 1, 3, 10, and 30 μM
Incubation Time: 24 h
Result: Had a low inhibitory effect on cell viability of HEK293T cells (68%).
Parmacokinetics[1]
Species Dose Route Indicator value
Mice 1 mg/kg i.v. Cmax 264 ng/mL
Mice 10 mg/kg p.o. Cmax 328 ng/mL
Mice 1 mg/kg i.v. Tmax 0.083 hr
Mice 10 mg/kg p.o. Tmax 0.75 hr
Mice 1 mg/kg i.v. T1/2 0.59 hr
Mice 10 mg/kg p.o. T1/2 1.2 hr
Mice 1 mg/kg i.v. AUC0-t 181 ng·h/mL
Mice 10 mg/kg p.o. AUC0-t 820 ng·h/mL
Mice 1 mg/kg i.v. AUC0-inf 183 ng·h/mL
Mice 10 mg/kg p.o. AUC0-inf 825 ng·h/mL
Mice 1 mg/kg i.v. CL 91 mL/min/kg
Mice 10 mg/kg p.o. MRT0-t 2.0 hr
Mice 1 mg/kg i.v. MRT0-t 0.66 hr
Mice 10 mg/kg p.o. F 45 %
Mice 1 mg/kg i.v. Vss 0.0036 L/kg
In Vivo

PLK1-IN-12 (Compound B31) (10/20 mg/kg, i.g., twice weekly for 11 d) can inhibit tumor growth in a mouse subcutaneous K562 cell transplantation tumor model[1].
PLK1-IN-12 (500 mg/kg, i.g., once daily for 7 d) has no tissue damage or toxicity to various organs of mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Subcutaneous K562 cell transplantation tumor model, Male BALB/c mice (6–8 weeks old, weighing 18–20 g)[1]
Dosage: 10/20 mg/kg
Administration: Intragastric (i.g.), twice weekly for 11 d
Result: Inhibited tumor growth.
Animal Model: Acute toxicity test[1]
Dosage: 500 mg/kg
Administration: Intragastric (i.g.), once daily for 7 d
Result: Compared with the mice in the positive control group, there was no significant change in body weight, and no obvious damage to the heart, kidney, lung, liver and spleen.
Molecular Weight

558.12

Formula

C28H40ClN7O3
SMILES

CN(C1=O)C(C=NC(NC2=C(C(Cl)=CC(N3CCN(CC3)C)=C2)OCCCO)=N4)=C4N([C@@H]1CC)C5CCCC5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PLK1-IN-12 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PLK1-IN-12Polo-like Kinase (PLK)Anti-cancerH460 cell linesA549 cell linesSW620 cell linesHL-60 cell linesK562 cell linesCCRF-CEM cell linessubcutaneous K562 cell transplantation tumor modelAnti-leukemiaInhibitorinhibitorinhibit

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