127228-54-0
127228-54-0 结构式
物理化学性质
密度1.68±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度溶于二甲基亚砜
酸度系数(pKa)3.50±0.10(Predicted)
形态Solid
颜色White to off-white
常见问题列表
生物活性
LY309887 是一种有效的二氢叶酸还原酶 (GARFT) 抑制剂，Ki 值为 6.5 nM，具有抗肿瘤活性。靶点
Ki: 6.5 nM (GARFT), 1.78 nM (Folate receptor α), 18.2 nM (Folate receptor β)
体外研究
LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a K i of 6.5 nM for human GARFT and also has high affinity at human folate receptor (FR)α and FRβ (K i , 1.78 nM and 18.2 nM, respectively). LY309887 is signigicantly cytotoxic against the human leukemia cell line CCRF-CEM with IC 50 of 9.9 nM.
体内研究
LY309887 (3 mg/kg-100 mg/kg, i.p.) shows complete inhibition on the tumor growth in mice bearing C3H mammary cancer cells.