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| Targets |
TC-S 7005 targets Polo-like kinases (Plks), specifically PLK2, PLK3, and PLK1. Plks are serine/threonine kinases that play essential roles in cell cycle regulation, particularly during mitosis. By inhibiting Plks, TC-S 7005 disrupts cell cycle progression and may have antiproliferative effects. The compound shows selectivity for PLK2 over PLK1 and PLK3 in cell-free assays.
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| ln Vitro |
Myofibroblast secretion is strongly increased and the rate of fibroblast proliferation is decreased by TC-S 7005 [2].
In vitro, TC-S 7005 is a PLK inhibitor with IC50 values of 4 nM for PLK2, 24 nM for PLK3, and 214 nM for PLK1. In human SR fibroblasts, TC-S 7005 (1 μM) significantly promotes myofibroblast differentiation and reduces fibroblast proliferation rate. The compound's activity is assessed in kinase inhibition assays and cell-based proliferation assays. |
| ln Vivo |
In vivo, TC-S 7005 is used as a research tool to study the role of Plks in cell cycle regulation and proliferation. By inhibiting PLK2, the compound may affect cell cycle progression and have potential applications in cancer research. Detailed in vivo data are available in research publications.
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| Enzyme Assay |
In vitro enzyme assays for TC-S 7005 measure its inhibition of PLK1, PLK2, and PLK3 activity. The kinase is incubated with its substrate and ATP in the presence of varying concentrations of the compound. Kinase activity is measured by quantifying substrate phosphorylation using radioactive or fluorescence-based methods. IC50 values of 214 nM, 4 nM, and 24 nM are determined for PLK1, PLK2, and PLK3, respectively.
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| Cell Assay |
Cell proliferation analysis [2]
Cell Types: primary human SR fibroblasts Tested Concentrations: 1 μM Incubation Duration: 7 days Experimental Results: Dramatically induced myofibroblast differentiation and diminished fibroblast proliferation rate. In vitro cell-based assays for TC-S 7005 use fibroblast or cancer cell lines to assess its effects on cell proliferation and differentiation. Cells are treated with serial dilutions of the compound, and cell proliferation is measured using MTT or other assays. Myofibroblast differentiation is assessed by measuring α-SMA expression or other differentiation markers. |
| Animal Protocol |
In vivo animal models for TC-S 7005 include models where Plk inhibition is relevant, such as cancer models. The compound is administered via appropriate routes, and its effects on tumor growth, cell cycle progression, and disease progression are evaluated. Pharmacodynamic studies measure Plk inhibition in target tissues.
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| ADME/Pharmacokinetics |
TC-S 7005 has a molecular formula of C21H17N3O3 and a molecular weight of 359.38 g/mol. It is an isoxazolopyridine-class compound and has the chemical name 3-(2H-1,3-benzodioxol-5-yl)-N-[(1S)-1-phenylethyl]-[1,2]oxazolo[5,4-c]pyridin-5-amine. The compound has a purity of ≥98% and is stored under appropriate conditions for research use.
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| Toxicity/Toxicokinetics |
The toxicity profile of TC-S 7005 is characterized in preclinical safety studies. As a Plk inhibitor, the compound may affect cell cycle progression and proliferation. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
TC-S 7005 is a potent inhibitor of Polo-like kinases (Plks) with IC50 values of 4 nM for PLK2, 24 nM for PLK3, and 214 nM for PLK1. It is an isoxazolopyridine-class compound and shows selectivity for PLK2 over PLK1 and PLK3. TC-S 7005 promotes myofibroblast differentiation and reduces fibroblast proliferation. It is intended for laboratory research use only.
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| Molecular Formula |
C21H17N3O3
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|---|---|
| Molecular Weight |
359.377984762192
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| Exact Mass |
359.127
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| CAS # |
1082739-92-1
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| PubChem CID |
24971422
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
501
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O1C2C=NC(=CC=2C(C2=CC=C3C(=C2)OCO3)=N1)N[C@@H](C)C1C=CC=CC=1
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| InChi Key |
DAAGOCSHXCDWDY-ZDUSSCGKSA-N
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| InChi Code |
InChI=1S/C21H17N3O3/c1-13(14-5-3-2-4-6-14)23-20-10-16-19(11-22-20)27-24-21(16)15-7-8-17-18(9-15)26-12-25-17/h2-11,13H,12H2,1H3,(H,22,23)/t13-/m0/s1
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| Chemical Name |
3-(1,3-benzodioxol-5-yl)-N-[(1S)-1-phenylethyl]-[1,2]oxazolo[5,4-c]pyridin-5-amine
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| Synonyms |
TCS 7005; TC S 7005; TC-S 7005
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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 : ~125 mg/mL (~347.82 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 | 2.7826 mL | 13.9128 mL | 27.8257 mL | |
| 5 mM | 0.5565 mL | 2.7826 mL | 5.5651 mL | |
| 10 mM | 0.2783 mL | 1.3913 mL | 2.7826 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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