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.
- CAS No.: 3038489-48-1
- Formula: C29H39N9O2S
- Molecular Weight:577.74
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PLK1 0.27 nM (IC50) |
PLK2 12.72 nM (IC50) |
PLK3 4.12 nM (IC50) |
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.
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Cell Line:MV4-11 cells
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Concentration:2.92 nM, 5.83 nM, 11.6 nM, 23.3 nM, and 46.6 nM
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Incubation Time:72 h
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Result:Increased the cell apoptosis rate, ranging from 3.29% to 67.7% in a concentration-dependent manner.
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.
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Animal Model:subcutaneous xenograft mouse models of MV4-11, Balb/c nude mice [1]
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Dosage:20 mg/kg
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Administration:p.o., once a day for 19 consecutive days.
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Result:Inhibited the tumor growth (TGI=91.2%).
Showed no significant weight loss or death in mice.
Chemical Information
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CAS No. 3038489-48-1
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Molecular Weight 577.74
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Formula C29H39N9O2S
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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
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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)
PLK1-IN-13 Related Classifications
HY-173212 Related Classifications
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