| Bioactivity | 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]. |
| Invitro | KIN59 (0-100 µM; 24 h) 抑制细胞增殖，对 FGF2 (30 ng/mL) 和 PBS (10%) 刺激的 GM7373 细胞的 IC50 值分别为 5.8 和 63 µM[1].KIN59 (60 µM; 30 min) 抑制 FGF2 （10 ng/mL）刺激的 FGFR1 过表达 GM7373-FGFR1 细胞中 p-FGFR1、P-Akt 的表达[1]。KIN59 抑制重组细菌 (大肠杆菌) 和人胸苷磷酸化酶 (TPase)，IC50 值分别为 44 μM 和 67 μM[2]。 Cell Proliferation Assay[1] Cell Line: |
| In Vivo | KIN59 (15 mg/kg；皮下注射；从第 2 天开始每天两次，持续 20 天) 在小鼠体内显示出抗肿瘤活性[1]。 Animal Model: |
| Name | KIN59 |
| CAS | 4152-77-6 |
| Formula | C29H26N4O5 |
| Molar Mass | 510.54 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| 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. |