SML0586
Lomeguatrib
≥98% (HPLC)
Synonym(s):
2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine, O6-(4-bromothenyl)guanine
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About This Item
Empirical Formula (Hill Notation):
C10H8BrN5OS
CAS Number:
Molecular Weight:
326.17
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
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)
SMILES string
Nc1nc(OCc2cc(Br)cs2)c3nc[nH]c3n1
InChI key
JUJPKFNFCWJBCX-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 10 mg/mL, clear
storage temp.
room temp
Quality Level
Related Categories
Biochem/physiol Actions
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).
signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Malcolm Ranson et al.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 25(18), 2540-2545 (2007-06-20)
To evaluate tumor response, pharmacodynamic effects, and safety of a combination of lomeguatrib (LM), an O6-methylguanine DNA-methyltransferase (MGMT) inactivator, and temozolomide (TMZ), TMZ alone, and LM/TMZ after disease progression on TMZ alone in patients with advanced melanoma. Patients with unresectable
[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)
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))
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
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
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