产品
编 号:F352846
分子式:C29H26N4O5
分子量:510.54
产品类型
结构图
CAS No: 4152-77-6
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产品详情
生物活性:
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.
体内研究:
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。Animal Model:Eight-week-old female, 25 g, athymic, nude nu/nu mice (F2T-luc2.9 cellss)
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.
体外研究:
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.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。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。