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化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 10 mg/mL, clear
儲存溫度
room temp
SMILES 字串
Nc1nc(OCc2cc(Br)cs2)c3nc[nH]c3n1
InChI
1S/C10H8BrN5OS/c11-5-1-6(18-3-5)2-17-9-7-8(14-4-13-7)15-10(12)16-9/h1,3-4H,2H2,(H3,12,13,14,15,16)
InChI 密鑰
JUJPKFNFCWJBCX-UHFFFAOYSA-N
生化／生理作用
Lomeguatrib is a highly potent inactivator of O(6)-methylguanine-DNA methyltransferase (MGMT), a DNA repair protein which can confer resistance to some cancer chemotherapeutics, in particular the DNA alkylating agents such as Temozolomide, DTIC, Carmustine, etc. Lomeguatrib is a highly potent inactivator of MGMT and can be used to further investigate mechanisms of resistance. It is a potent irreversible inactivator of all mammalian O6-alkylguanine-DNA-alkyltransferases, so far tested with nanomolar activity in vitro and in vivo.
Lomeguatrib is a highly potent irreversible inactivator of O(6)-methylguanine-DNA methyltransferase (MGMT).
訊號詞
Warning
危險聲明
危險分類
Acute Tox. 4 Oral
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
Patrizia Caporaso et al.
DNA repair, 6(8), 1179-1186 (2007-05-15)
Previous studies indicated that dacarbazine and Temozolomide could be highly effective against refractory acute leukaemia. Their activity relies mainly on the generation of methyl adducts at the O(6)-position of guanine in DNA. High levels of O(6)-methylguanine-DNA methyltransferase (MGMT) or a
A Sabharwal et al.
Cancer chemotherapy and pharmacology, 66(5), 829-835 (2009-12-30)
Expression of the DNA repair protein O (6)-methylguanine-DNA methyltransferase (MGMT) correlates with resistance to irinotecan in colorectal cancer cell lines. This phase I study evaluated the maximum tolerated dose (MTD) of lomeguatrib, an inactivating pseudosubstrate of MGMT, in combination with
O A Khan et al.
British journal of cancer, 98(10), 1614-1618 (2008-05-14)
To evaluate the tumour response to lomeguatrib and temozolomide (TMZ) administered for 5 consecutive days every 4 weeks in patients with metastatic colorectal carcinoma. Patients with stage IV metastatic colorectal carcinoma received lomeguatrib (40 mg) and TMZ (50-200 mg m(-2))
[Analysis of the relevant factors of mechanism for telozolomide chemoresistance].
Zeng-feng Sun et al.
Zhonghua zhong liu za zhi [Chinese journal of oncology], 33(10), 794-796 (2012-02-18)
T Brian H McMurry
DNA repair, 6(8), 1161-1169 (2007-05-09)
The DNA repair protein, O(6)-alkylguanine-DNA alkyltransferase (MGMT) can confer resistance to the cancer chemotherapeutic effects of the class of DNA damaging drugs generally referred to as the O(6)-alkylating agents. Inactivation of MGMT is thus a practical approach to improving the
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