产品
编 号:F067878
分子式:C23H21N5
分子量:367.45
产品类型
结构图
CAS No: 1200126-26-6
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产品详情
生物活性:
GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 μM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity.
体内研究:
GNE-900 (2.5-40 mg/kg; p.o.; once) 与gemcitabine (HY-17026) 联用能降低肿瘤体积并增加 DNA 损伤和 γ-H2AX 的表达水平在大鼠中。Animal Model:Sprague-Dawley rats (HT-29 tumor xenografts)
Dosage:2.5-40 mg/kg (received a dose of gemcitabine 120 mg/kg)
Administration:P.o.; once
Result:Decreased the tumor volume and resulted in significant enhancement of DNA damage, increased γ-H2AX levels.
体外研究:
GNE-900 (1 μM; 1-48 h) 在 HT-29 细胞中与吉西他滨 (50 nM) 联合使用时,可诱导细胞凋亡并增加裂解的 PARP 的表达。