| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
PLK4 7.9 nM (IC50)
PLK4-IN-4 targets polo-like kinase 4 (PLK4), a serine/threonine protein kinase that plays a critical role in centriole biogenesis and cell division. The compound inhibits PLK4 with an IC50 value of 7.9 nM. PLK4 is essential for the duplication of centrioles, which are key components of the centrosome involved in mitotic spindle organization. Dysregulation of PLK4 is associated with cancer, making it a potential therapeutic target. |
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| ln Vitro |
In vitro studies demonstrate that PLK4-IN-4 is a potent inhibitor of PLK4 with an IC50 value of 7.9 nM. This high potency indicates strong inhibitory activity against the kinase. By inhibiting PLK4, the compound disrupts centriole duplication, which is essential for proper cell division. The compound has been investigated for its potential in cancer research. Detailed cellular activity data, including IC50 values in cancer cell lines, are not extensively documented in the available literature.
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| ln Vivo |
In vivo activity of PLK4-IN-4 is inferred from its potential use in cancer research. As an inhibitor of PLK4, a critical regulator of centriole biogenesis and cell division, the compound is expected to have antitumor activity by disrupting mitotic progression. Detailed in vivo efficacy data from animal models, including tumor growth inhibition studies, are not extensively documented in the available literature. The compound is intended for research use only.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for PLK4-IN-4 involves measuring its inhibitory activity against polo-like kinase 4 (PLK4). The assay typically uses purified recombinant PLK4 enzyme incubated with the compound at varying concentrations, along with ATP and a peptide substrate. Kinase activity is measured by quantifying phosphorylation levels using methods such as radiometric assays, fluorescence polarization, or ELISA-based detection. The IC50 value of 7.9 nM is determined by plotting percentage inhibition against compound concentration.
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| Cell Assay |
In vitro cell-based assays for PLK4-IN-4 are conducted using cancer cell lines to evaluate its antiproliferative effects. Cells are treated with the compound at various concentrations, and cell viability is measured using MTT or CCK-8 assays. The effect on cell cycle progression and mitotic defects is assessed by flow cytometry and immunofluorescence microscopy of centrosome and spindle structures. Apoptosis induction is evaluated by measuring caspase activation or Annexin V staining.
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| Animal Protocol |
In vivo animal studies for PLK4-IN-4 are typically conducted using xenograft mouse models implanted with cancer cells. Tumor-bearing mice are administered the compound via appropriate routes at various doses, and tumor growth inhibition is monitored. Pharmacokinetic parameters are determined from plasma samples. Tolerability is assessed by monitoring body weight changes and clinical signs. Efficacy is evaluated by measuring tumor volume, weight, and histological examination.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of PLK4-IN-4 include a molecular weight of 439.46 and a molecular formula of C21H23F2N9. Purity is reported as 99.89%. Detailed pharmacokinetic parameters such as solubility, half-life, and bioavailability are not extensively documented in the available literature. The compound is intended for research use only. Storage and formulation details are not provided in the search results.
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| Toxicity/Toxicokinetics |
Toxicity information for PLK4-IN-4 is limited in the available literature. Standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only and is not for human therapeutic applications. Cytotoxicity should be evaluated in cell-based assays to determine the therapeutic window. No detailed toxicity data are available from the search results.
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| References | |
| Additional Infomation |
PLK4-IN-4 (compound 22) is a potent inhibitor of polo-like kinase 4 (PLK4) with an IC50 value of 7.9 nM. PLK4 is a critical regulator of centriole biogenesis and cell division. By inhibiting PLK4, the compound disrupts centriole duplication, making it a valuable tool for cancer research. It has the potential for the research of cancer. It is intended for research use only.
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| Molecular Formula |
C21H23F2N9
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|---|---|
| Molecular Weight |
439.46
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| Exact Mass |
439.204
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| CAS # |
2923999-01-1
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| PubChem CID |
168279678
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| Appearance |
White to yellow solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
32
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| Complexity |
610
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC(=NN1)NC2=C3C=NN(C3=NC(=N2)NCC4=C(C=C(C=C4)F)F)C5CCNCC5
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| InChi Key |
HPYJNDCKRXOAKV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H23F2N9/c1-12-8-18(31-30-12)27-19-16-11-26-32(15-4-6-24-7-5-15)20(16)29-21(28-19)25-10-13-2-3-14(22)9-17(13)23/h2-3,8-9,11,15,24H,4-7,10H2,1H3,(H3,25,27,28,29,30,31)
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| Chemical Name |
6-N-[(2,4-difluorophenyl)methyl]-4-N-(5-methyl-1H-pyrazol-3-yl)-1-piperidin-4-ylpyrazolo[3,4-d]pyrimidine-4,6-diamine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
Typically soluble in DMSO (e.g. 10 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.69 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.69 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2755 mL | 11.3776 mL | 22.7552 mL | |
| 5 mM | 0.4551 mL | 2.2755 mL | 4.5510 mL | |
| 10 mM | 0.2276 mL | 1.1378 mL | 2.2755 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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