LY309887
| 中文名称 | LY309887 |
|---|---|
| 中文同义词 | 化合物 T15813 |
| 英文名称 | LY309887 |
| 英文同义词 | LY309887;GQCXGHHHNACOGE-SKDRFNHKSA-N;LY309887,LY-309887;L-Glutamic acid, N-[[5-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]-2-thienyl]carbonyl]- |
| CAS号 | 127228-54-0 |
| 分子式 | C19H23N5O6S |
| 分子量 | 449.48 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 127228-54-0.mol |
| 结构式 |  |
LY309887 性质
| 密度 | 1.68±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 固体 |
| 酸度系数(pKa) | 3.50±0.10(Predicted) |
| 颜色 | 白色至米白色 |
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。
Ki: 6.5 nM (GARFT), 1.78 nM (Folate receptor α), 18.2 nM (Folate receptor β)
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.
LY309887 (3 mg/kg-100 mg/kg, i.p.) shows complete inhibition on the tumor growth in mice bearing C3H mammary cancer cells.