S84175 |
Lomeguatrib |
源葉(MedMol) | ≥98% |
- 產(chǎn)品描述: Lomeguatrib is a O6-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC50s of 9 nM in cell-free assay and ~6?nM in MCF-7 cells.
- 靶點: MGMTcc:6 nM (IC50, in MCF-7 cells);MGMT:9 nM (IC50);DNAMethyltransferase;?DNAAlkylation
- 體外研究:
Lomeguatrib (Compound 10) is a O6-methylguanine methyltransferase (MGMT) inhibitor, with an IC50 of 9 nM in cell-free assay and ~6?nM in MCF-7 cells. Lomeguatrib (10?μM) substantially increases the growth inhibitory effects of temozolomide in MCF-7 cells (D60=10?μM with Lomeguatrib vs 400?μM without)
- 體內(nèi)研究:
Lomeguatrib (20?mg/kg i.p.) completely inactivates MGMT within 2?h, but shows no significant effect on tumor growth in MCF-7 xenografts
- 參考文獻(xiàn):
1. Reinhard J, et al. Monosaccharide-linked inhibitors of O(6)-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships. J Med Chem. 2001 Nov 22;44(24):4050-61. 2. Clemons M, et al. O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts. Br J Cancer. 2005 Nov 14;93(10):1152-6.
- 溶解性: soluble in DMSO
- 保存條件: 2-8℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 3.066 ml 15.329 ml 30.659 ml 5 mM 0.613 ml 3.066 ml 6.132 ml 10 mM 0.307 ml 1.533 ml 3.066 ml 50 mM 0.061 ml 0.307 ml 0.613 ml
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質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)