4152-77-6

4152-77-6 structure
4152-77-6 structure
  • Name: 5’O-Tritylinosine
  • Chemical Name: 5'-O-tritylinosine
  • CAS Number: 4152-77-6
  • Molecular Formula: C29H26N4O5
  • Molecular Weight: 510.54100
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage Nucleoside Antimetabolite/Analog
  • Create Date: 2016-10-14 06:46:16
  • Modify Date: 2025-08-25 10:17:57
  • 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].

Name 5'-O-tritylinosine
Synonyms 5'-O-Tritylinosine
5’O-Tritylinosine
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].
Related Catalog
In Vitro 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: 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;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: 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.
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.  

Molecular Formula C29H26N4O5
Molecular Weight 510.54100
Exact Mass 510.19000
PSA 122.49000
LogP 2.74750
Storage condition 2-8℃
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