產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 10mg 50mg
CAS	192441-08-0
別名
化學名	6-[(4-bromothiophen-2-yl)methoxy]-7H-purin-2-amine
分子式	C10H8BrN5OS
分子量	326.17
溶解度	≥ 50mg/mL in DMSO with gentle warming
儲存條件	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

產(chǎn)品描述：

Lomeguatrib is an O6-methylguanine-DNA-methyl-transferase (MGMT) inhibitor [1], with an IC50 value of about 6 nM to inactivate MGMT in MCF-7 cells, effectively [2].

MGMT activity is closely related to MTIC (a metabolite of dacarbazine)-mediated DNA damage [1].

Lomeguatrib sensitized MGMT-activity-bearing A375P cells to temozolomide (TMZ), but it failed to affect the effect of dacarbazine (DTIC). In other mutBRAF cells and several mutNRAS cell lines such as WM1361, similar results were obtained [1].

With one exception, patients treated with lomeguatrib showed no active or very low MGMT in PBMCs. Lomeguatrib at a dose of 20 mg resulted in 16.7 fmol/μg DNA active MGMT in a CNS-tumor-bearing patient. This patient showed a percentage of 25% for inactive tumor MGMT. This percentage was lower than that in the other two CNS patients with lomeguatrib at the same dose. Different tumor types showed remarkable differences in total tumor MGMT. Prostate cancers had the highest (554 ± 404 fmol/mg protein), CNS tumors had the lowest (89.9 ± 44.5 fmol/mg protein), and colorectal tumors had intermediate levels of total protein (244 ± 181 fmol/mg protein). In the colorectal cancer, the primary CNS tumor, and the prostate cancer of patients, increasing lomeguatrib doses resulted in increasing inactive MGMT proportions [3].

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1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術有限公司

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