Pemetrexed (sodium salt hydrate) 是一种新型抗叶酸剂，LY231514 的五谷氨酸的 Ki 值分别为 1.3、7.2 和 65 nM，用于抑制胸苷酸合成酶 (TS)、二氢叶酸还原酶 (DHFR) 和甘氨酰胺核糖核苷酸甲酰转移酶 (GARFT) .
| Cas No. | 357166-29-1 |
| 别名 | 培美曲赛二钠七水合物,LY231514 disodium heptahydrate |
| Canonical SMILES | O=C(N[C@H](C([O-])=O)CCC([O-])=O)C(C=C1)=CC=C1CCC2=CNC(NC(N)=N3)=C2C3=O.[Na+].[Na+].O.O.O.O.O.O.O |
| 分子式 | C20H19N5O6•2Na [7H2O] |
| 分子量 | 597.5 |
| 溶解度 | PBS (pH 7.2): 10 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Pemetrexed is pyrrotopyrimidine-based, multi-targeted antifolate with broad in vivo antitumor activity. Originally identified as a highly efficient substrate for folylpolyglutamate synthase, pemetrexed potently inhibits multiple folate-dependent enzymes involved in both purine and pyrimidine synthesis including thymidylate synthase (Ki = 109 nM), dihydrofolate reductase (Ki = 7 nM), glycinamide ribonucleotide formyltransferase (Ki = 9.3 μM), and aminoimidazole carboxamide ribonucleotide formyltransferase (Ki = 3.6 μM). Its antiproliferative activity has been demonstrated in a wide variety of solid tumors, including non-small cell lung, breast, mesothelioma, colorectal, pancreatic, gastric, bladder, cervix, and head and neck. |
