127228-54-0
127228-54-0 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
密度1.68±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)3.50±0.10(Predicted)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
LY309887 是一種有效的二氫葉酸還原酶 (GARFT) 抑制劑，Ki 值為 6.5 nM，具有抗腫瘤活性。靶點(diǎn)
Ki: 6.5 nM (GARFT), 1.78 nM (Folate receptor α), 18.2 nM (Folate receptor β)
體外研究
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.
體內(nèi)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.