Lomeguatrib
Cat. No.：YN310236
CAS No. ：192441-08-0
| 产品名称: | Lomeguatrib |
| CAS No.: | 192441-08-0 |
| Chemical Name: | 6-[(4-bromo-2-thienyl)methoxy]-9H-purin-2-amine |
| Synonyms: | PaTrin-2 |
| 分子量: | 326.17 |
| 分子式: | C₁₀H₈BrN₅OS |
| SMILES: | NC1=NC(OCC2=CC(Br)=CS2)=C3N=CNC3=N1 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Lomeguatrib 是一种有效的MGMT抑制剂，在非细胞体系和 MCF-7 细胞体系中，IC50值分别为 9 nM 和 ∼6 nM。 |
| IC50和靶点: | [{name:"MGMT:6 nM (IC50, in MCF-7 cells)"},{name: "MGMT:9 nM (IC50)"}] |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
McMurry, T.B.H.MGMT inhibitors-the Trinity College-Paterson Institute experience, a chemist's perceptionDNA Repair6(8),1161-1169(2007)
Clemons, M., Kelly, J., Watson, A.J., et al.O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenograftsBr. J. Cancer93(10),1152-1156(2005)
Marchesi, F., Turriziani, M., Tortorelli, G., et al.Triazene compounds: Mechanism of action and related DNA repair systemsPharmacol. Res.56(4),275-287(2007)
Ranson, M., Middleton, M.R., Bridgewater, J., et al.Lomeguatrib, a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase: Phase I safety, pharmacodynamic, and pharmacokinetic trial and evaluation in combination with temozolomide in patients with advanced solid tumorsClin. Cancer Res.12(5),1577-1584(2006)
Watson, A.J., Sabharwal, A., Thorncroft, M., et al.Tumor O6-methylguanine-DNA methyltransferase inactivation by oral lomeguatribClin. Cancer Res.16(2),743-749(2010)
