For research use only. Not for therapeutic Use.
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].
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].
KIN59 (15 mg/kg; s.c.; twice daily from day 2 for 20 days) shows anti-tumor activity in mice[1].
| Catalog Number | R041768 |
| CAS Number | 4152-77-6 |
| Synonyms | 9-[(2R,3S,5R)-3,4-dihydroxy-5-(trityloxymethyl)oxolan-2-yl]-1H-purin-6-one |
| Molecular Formula | C29H26N4O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C29H26N4O5/c34-24-22(38-28(25(24)35)33-18-32-23-26(33)30-17-31-27(23)36)16-37-29(19-10-4-1-5-11-19,20-12-6-2-7-13-20)21-14-8-3-9-15-21/h1-15,17-18,22,24-25,28,34-35H,16H2,(H,30,31,36)/t22-,24?,25+,28-/m1/s1 |
| InChIKey | YEPZMZDCXFRHCL-JYOIYRBNSA-N |
| SMILES | C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3)OCC4C(C(C(O4)N5C=NC6=C5N=CNC6=O)O)O |
| Reference | [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. |
