[CAS NO. 4152-77-6] KIN59
PRODUCTS SPECIFICATIONS [4152-77-6]
DESCRIPTION [4152-77-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 510.54 |
| Molecular Formula | C29H26N4O5 |
| 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 |
Summary
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] .
In Vitro
KIN59 (0-100 µM; 24 h) inhibits GM7373 cell proliferative with IC
50
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 IC
50
values of 44 μM and 67 μM, respectively
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 IC 50 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] .
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. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
References
- [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.
- [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.