2. Cell Cycle/DNA Damage Apoptosis
  3. Polo-like Kinase (PLK) c-Myc Apoptosis
  4. PLK1-IN-13

PLK1-IN-13 is a selective and orally active PLK1 inhibitor (IC50: 0.27 nM). PLK1-IN-13 also inhibits PLK2 (IC50: 12.72 nM) and PLK3 (IC50: 4.12 nM). PLK1-IN-13 arrests cell at G2 phase, induces apoptosis and down-regulates the transcription of the proliferation-related oncogene c-MYC. PLK1-IN-13 inhibits tumor growth, and can be used for research of acute myeloid leukemia (AML).

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

PLK1-IN-13 Chemical Structure

PLK1-IN-13 Chemical Structure

CAS No. : 3038489-48-1

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PLK1-IN-13 Related Antibodies

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Description

PLK1-IN-13 is a selective and orally active PLK1 inhibitor (IC50: 0.27 nM). PLK1-IN-13 also inhibits PLK2 (IC50: 12.72 nM) and PLK3 (IC50: 4.12 nM). PLK1-IN-13 arrests cell at G2 phase, induces apoptosis and down-regulates the transcription of the proliferation-related oncogene c-MYC. PLK1-IN-13 inhibits tumor growth, and can be used for research of acute myeloid leukemia (AML)[1].

IC50 & Target[1]

PLK1

0.27 nM (IC50)

PLK2

12.72 nM (IC50)

PLK3

4.12 nM (IC50)

In Vitro

PLK1-IN-13 (Compound WD6) (72 h) has antiproliferative activities against MDA-MB-231 (IC50: 9.5 nM) and MV4-11 cell (IC50: 23.3 nM), and the IC50 for MCF-7 and HCT-116 are 47.1 nM and 59.9 nM respectively[1].
PLK1-IN-13 has weak inhibitory effects on CYP2C9 (IC50: 7.39 μM), CYP2C19 (IC50: 14 μM), CYP2D6 (IC50: 13.8 μM), and CYP3A4 (IC50: 17.3 μM), indicating that PLK1-IN-13 may have lower drug-drug interactions[1].
PLK1-IN-13 (2.92 nM-46.6 nM, 72 h) induces G2/M cell-cycle arrest and induces apoptosis in MV4-11 cells[1].
PLK1-IN-13 (0-1 μM, 24 h) down-regulates the transcription of the proliferation-related oncogene c-MYC in MV4-11 cells[1].

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

PLK1-IN-13 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 2.92 nM, 5.83 nM, 11.6 nM, 23.3 nM, and 46.6 nM
Incubation Time: 72 h
Result: Increased the cell apoptosis rate, ranging from 3.29% to 67.7% in a concentration-dependent manner.
Parmacokinetics[1]
Species Dose Route Indicator value
Rat 1 mg/kg i.v. T1/2 5.82 hr
Rat 10 mg/kg i.g. T1/2 7.59 hr
Rat 1 mg/kg i.v. AUC0-t 8.35 μg·h/mL
Rat 10 mg/kg i.g. Tmax 5.53 hr
Rat 10 mg/kg i.g. Cmax 1900 ng/mL
Rat 10 mg/kg i.g. AUC0-t 29.3 μg·h/mL
In Vivo

PLK1-IN-13 (Compound WD6) (20 mg/kg, p.o., once a day for 19 consecutive days) inhibits the tumor growth (TGI = 91.2 %) in xenograft mouse models of MV4-11[1].
PLK1-IN-13 (10, 20 mg/kg, i.g.) shows a good half-life, high plasma exposure, and moderate bioavailability in SD rats[1].

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

Animal Model: subcutaneous xenograft mouse models of MV4-11, Balb/c nude mice [1]
Dosage: 20 mg/kg
Administration: p.o., once a day for 19 consecutive days.
Result: Inhibited the tumor growth (TGI=91.2%).
Showed no significant weight loss or death in mice.
Molecular Weight

577.74

Formula

C29H39N9O2S
CAS No.
SMILES

O=C1N(C)C2=CN=C(NC3=CC=C(C4=NN=C(CN5CCN(C)CC5)S4)C=C3OC)N=C2N(C6CCCC6)[C@@H]1CC
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-13 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-133038489-48-1Polo-like Kinase (PLK)c-MycApoptosisMycAcute myeloid leukemiaAMLMV4-11cell-cycle arrestc-mycInhibitorinhibitorinhibit

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