2. Cell Cycle/DNA Damage
  3. Nucleoside Antimetabolite/Analog
  4. KIN59

KIN59  (Synonyms: 5'-O-Tritylinosine; 5'-O-Trityl-inosine)

Cat. No.: HY-102071 Purity: ≥99.0%
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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.

For research use only. We do not sell to patients.

KIN59 Chemical Structure

KIN59 Chemical Structure

CAS No. : 4152-77-6

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Customer Review

Based on 1 publication(s) in Google Scholar

KIN59 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

Cellular Effect
Cell Line Type Value Description References
Vero CC50
30 μM
Compound: 5a
Cytotoxicity against african green monkey Vero cells after 1 week
Cytotoxicity against african green monkey Vero cells after 1 week
[PMID: 23721953]
In Vitro

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.

KIN59 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: GM7373 cells
Concentration: 0-100 µM
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: GM7373-FGFR1, GM7373-VEGFR2 cells
Concentration: 60 µM
Incubation Time: 30 min
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.
In Vivo

KIN59 (15 mg/kg; s.c.; twice daily from day 2 for 20 days) shows anti-tumor activity in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Eight-week-old female, 25 g, athymic, nude nu/nu mice (F2T-luc2.9 cellss)[1]
Dosage: 15 mg/kg
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
Result: Caused a significant inhibition in the rate of tumor growth.
Molecular Weight

510.54

Formula

C29H26N4O5
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9587 mL 9.7936 mL 19.5871 mL
5 mM 0.3917 mL 1.9587 mL 3.9174 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2 mg/mL (3.92 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: ≥99.0%

SDS (252 KB)

COA (260 KB)

Handling Instructions (2659 KB)
References

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
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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KIN59 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KIN594152-77-65'-O-Tritylinosine 5'-O-Trityl-inosineKIN 59KIN-59Nucleoside Antimetabolite/AnalogGM7373 cellsp-FGFR1,P-Aktanti-tumorFGF2Inhibitorinhibitorinhibit

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