135503-67-2
135503-67-2 結(jié)構(gòu)式
基本信息
中文別名
化合物 T11922 英文別名
LY 254155GQCXGHHHNACOGE-ACGXKRRESA-N
L-Glutamic acid, N-[[5-[2-(2-amino-1,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl)ethyl]-2-thienyl]carbonyl]- (9CI)
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)
常見(jiàn)問(wèn)題列表
生物活性
LY 254155 是一種抗葉酸劑。LY 254155 抑制 hGARFT 及與 mFBP 結(jié)合，Kis 分別為 2.1±0.2 和 1.7±0.1 nM。靶點(diǎn)
Ki: 2.1±0.2 (hGARFT ), 1.7± 0.1 nM (mFBP)
體外研究
LY 254155 inhibits recombinant human monofunctional glycinamide ribonucleotide formyltransferase (hGARFT) and binds to membrane folate-binding protein (mFBP) .
體內(nèi)研究
LY 254155 is active against a broad panel of murine and human xenograft solid tumors. LY 254155 (5, 10, 20, and 40 mg/kg) inhibits murine C3H carcinoma growth in C3H mice, with % inhibition of tumor growth is 49%, 71%, 90%, and 94%, respectively.