KIN59
Based on 1 Customer Validation
KIN59 (5’-O-Tritylinosine) is a potent thymidine phosphorylase allosteric inhibitor. KIN59 inhibits FGF2-stimulated cell growth. KIN59 inhibits the expression of p-FGFR1, P-Akt in FGF2 (10 ng/mL) stimulated cells. KIN59 shows anti-tumor activity.
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- Pureté: 99.0%
- CAS No.: 4152-77-6
- Formule: C29H26N4O5
- Masse moléculaire:510.54
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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Cell Line
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Type | Value | Description | References |
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| Vero | CC50 |
30 μM
Compound: 5a
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Cytotoxicity against african green monkey Vero cells after 1 week
Cytotoxicity against african green monkey Vero cells after 1 week
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[PMID: 23721953] |
KIN59 (0-100 µM; 24 h) inhibits GM7373 cell proliferative with IC50 values of 5.8, 63 µM for FGF2 (30 ng/mL) and PBS (10%) stimulated, respectively[1].
KIN59 (60 µM; 30 min) inhibits the expression of p-FGFR1, P-Akt in FGF2 (10 ng/mL) stimited FGFR1-overexpressing GM7373-FGFR1 cells[1].
KIN59 inhibits recombinant bacterial (E. coli) and human thymidine phosphorylase (TPase) with IC50 values of 44 μM and 67 μM, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GM7373 cells
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Concentration:0-100 µM
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Incubation Time:24 h
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Result:Inhibited FGF2 (30 ng/mL)-induced proliferation of bovine macrovascular endothelial GM7373 cells in a dose-dependent manner with IC50 values of 5.8, 63 µM for FGF2 and PBS, respectively.
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Cell Line:GM7373-FGFR1, GM7373-VEGFR2 cells
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Concentration:60 µM
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Incubation Time:30 min
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Result:Inhibited FGFR1 phosphorylation and Akt activation triggered by FGF2 in FGFR1-overexpressing GM7373-FGFR1 cells, showed minor inhibits on VEGF-mediated VEGFR2 phosphorylation and Akt activation in GM7373 cells overexpressing VEGFR2.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Eight-week-old female, 25 g, athymic, nude nu/nu mice (F2T-luc2.9 cellss)[1]
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Dosage:15 mg/kg
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Administration:S.c.; twice daily from day 2 (once daily during the weekend) at a site distant from the tumor (inoculation) site for 20 days
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Result:Caused a significant inhibition in the rate of tumor growth.
Chemical Information
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CAS No. 4152-77-6
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Appearance Solid
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Masse moléculaire 510.54
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Formule C29H26N4O5
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Color White to off-white
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SMILES
O[C@H]1[C@@H](O)[C@H](N2C=NC3=C2N=CN=C3O)O[C@@H]1COC(C4=CC=CC=C4)(C5=CC=CC=C5)C6=CC=CC=C6
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Synonyms
5'-O-Tritylinosine; 5'-O-Trityl-inosine
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 16 mg/mL (31.34 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (3.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Liekens S, et al. The thymidine phosphorylase inhibitor 5'-O-tritylinosine (KIN59) is an antiangiogenic multitarget fibroblast growth factor-2 antagonist. Mol Cancer Ther. 2012 Apr;11(4):817-29. [Content Brief]
[2]. Liekens S, et al. Thymidine phosphorylase is noncompetitively inhibited by 5'-O-trityl-inosine (KIN59) and related compounds. Nucleosides Nucleotides Nucleic Acids. 2006;25(9-11):975-80. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9587 mL | 9.7936 mL | 19.5871 mL | 48.9678 mL |
| 5 mM | 0.3917 mL | 1.9587 mL | 3.9174 mL | 9.7936 mL | |
| 10 mM | 0.1959 mL | 0.9794 mL | 1.9587 mL | 4.8968 mL | |
| 15 mM | 0.1306 mL | 0.6529 mL | 1.3058 mL | 3.2645 mL | |
| 20 mM | 0.0979 mL | 0.4897 mL | 0.9794 mL | 2.4484 mL | |
| 25 mM | 0.0783 mL | 0.3917 mL | 0.7835 mL | 1.9587 mL | |
| 30 mM | 0.0653 mL | 0.3265 mL | 0.6529 mL | 1.6323 mL |
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