产品说明
应用
Lometrexol hydrate was used to compare the biological activity of potent inhibitor of human GARFTase.
包装
5, 25 mg in glass bottle
生化/生理作用
Glycinamide Ribonucleotide Formyltransferase (GARFTase) is a folate-dependent enzyme required for de novo purine synthesis. Lometrexate is a potent inhibitor of GARFTase, but does not interfere with enzymes involved in the synthesis of folate. Lometrexerol has been tested clinically for the treatment of various cancers as an anti-folate like agent, similar to methotrexate. Treatment with lometrexol rapidly decreases ATP and GTP levels, cell cycle arrest and induces apoptosis. Although depletion of nucleotide pools induces p53 expression, lometrexol is cytotoxic in both wild-type and mutant p53 expressing tumor cells. Lometrexol is cytotoxic in CCRF-CEm leukemia cells with an IC50 of 2.9 nM.
基本信息
| 经验(实验)分子式 | C21H25N5O6 · xH2O |
| 分子量 | 443.45 (anhydrous basis) |
| PubChem化学物质编号 | 329825110 |
产品性质
| 质量水平 | 100 |
| 测定 | ≥95% (HPLC) |
| 形式 | powder |
| 颜色 | white to light yellow |
| 溶解性 | DMSO: ≥5 mg/mL |
| 储存温度 | 2-8℃ |
| SMILES string | O.NC1=NC(=O)C2=C(NC[C@H](CCc3ccc(cc3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)C2)N1 |
| InChI | 1S/C21H25N5O6.H2O/c22-21-25-17-14(19(30)26-21)9-12(10-23-17)2-1-11-3-5-13(6-4-11)18(29)24-15(20(31)32)7-8-16(27)28;/h3-6,12,15H,1-2,7-10H2,(H,24,29)(H,27,28)(H,31,32)(H4,22,23,25,26,30);1H2/t12-,15+;/m1./s1 |
| InChI key | AEFQSKJUVDZANQ-YLCXCWDSSA-N |
安全信息
| 象形图 |  |
| 警示用语： | Danger |
| 危险声明 | H301 |
| 预防措施声明 | P301 + P310 |
| 危险分类 | Acute Tox. 3 Oral |
| 储存分类代码 | 6.1D - Non-combustible, acute toxic Cat.3 / toxic hazardous materials or hazardous materials causing chronic effects |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
