| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
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| Targets |
Cyclapolin-9 targets polo-like kinase 1 (PLK1), a serine/threonine-protein kinase that plays a critical role in cell cycle progression. It acts as an ATP-competitive inhibitor, binding to the ATP-binding site of PLK1 and preventing its activity. It is selective for PLK1 and is inactive against other kinases.
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| ln Vitro |
Cyclapolin 9 (3 μM) inhibits electrical field stimulation (EFS)-induced contraction of prostate strips. α1-adrenergic smooth muscle contraction in the human prostate can be reduced by Cyclapolin 9 [1].
Cyclapolin-9 is a potent inhibitor of PLK1 with an IC50 of 500 nM. It is selective for PLK1 and is inactive against other kinases. It acts as an ATP-competitive inhibitor. |
| ln Vivo |
In vivo activity data for Cyclapolin-9 is limited. As a potent and selective PLK1 inhibitor, it is expected to have effects on cell cycle progression and tumor growth. The compound is used as a research tool to study the role of PLK1 in cancer and other diseases.
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| Enzyme Assay |
Cyclapolin-9 is evaluated in cell-free kinase assays using purified PLK1. The compound is incubated with PLK1, ATP, and a substrate, and the inhibition of kinase activity is measured. IC50 values are determined to quantify the potency of PLK1 inhibition. Selectivity is assessed by screening against a panel of kinases.
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| Cell Assay |
Cyclapolin-9 is assessed in cell-based assays using cancer cell lines. Cells are treated with Cyclapolin-9, and cell cycle progression and proliferation are measured. The compound's ability to inhibit PLK1 activity in a cellular context is evaluated.
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| Animal Protocol |
Cyclapolin-9 is administered in animal models to evaluate its antitumor efficacy. However, specific animal study protocols are not extensively documented. The compound is typically formulated for in vivo administration using DMSO or other suitable vehicles.
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| ADME/Pharmacokinetics |
Cyclapolin-9 has a molecular weight of 307.21 and a molecular formula of C9H4F3N3O4S. It has a CAS number of 40533-25-3. The compound is soluble in DMSO at 20 mg/mL (with ultrasonic and warming and heat to 60°C). It should be stored in a cool, dry place.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Cyclapolin-9. The compound is for research use only and is not intended for human therapeutic use. Its safety profile has not been extensively characterized in the available literature.
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| References | |
| Additional Infomation |
Cyclapolin-9 is a potent, selective, and ATP-competitive PLK1 inhibitor. It has a CAS number of 40533-25-3. It is a natural product isolated from the marine sponge Cyclaptena sp.. It is used in cancer research. It is not approved for clinical use.
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| Molecular Formula |
C9H4F3N3O4S
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|---|---|
| Molecular Weight |
307.2
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| Exact Mass |
306.987
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| CAS # |
40533-25-3
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| PubChem CID |
2779952
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.579
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
430
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=C(C=C(C2=C1[N+](=C(S2)C(=O)N)[O-])[N+](=O)[O-])C(F)(F)F
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| InChi Key |
FHFLXKUKCSDMLD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H4F3N3O4S/c10-9(11,12)3-1-4-6(5(2-3)15(18)19)20-8(7(13)16)14(4)17/h1-2H,(H2,13,16)
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| Chemical Name |
7-nitro-3-oxido-5-(trifluoromethyl)-1,3-benzothiazol-3-ium-2-carboxamide
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| Synonyms |
Cyclapolin9; Cyclapolin 9; Cyclapolin-9
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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 |
| 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) |
DMSO : ~20 mg/mL (~65.10 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2552 mL | 16.2760 mL | 32.5521 mL | |
| 5 mM | 0.6510 mL | 3.2552 mL | 6.5104 mL | |
| 10 mM | 0.3255 mL | 1.6276 mL | 3.2552 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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