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SML0586

Sigma-Aldrich

Lomeguatrib

≥98% (HPLC)

Synonym(e):

2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine, O6-(4-bromothenyl)guanine

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About This Item

Empirische Formel (Hill-System):
C10H8BrN5OS
CAS-Nummer:
192441-08-0
Molekulargewicht:
326.17
MDL-Nummer:
MFCD23703756
UNSPSC-Code:
12352200
PubChem Substanz-ID:
329825566
NACRES:
NA.77

Assay

≥98% (HPLC)

Form

powder

Farbe

white to beige

Löslichkeit

DMSO: 10 mg/mL, clear

Lagertemp.

room temp

SMILES String

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)

InChIKey

JUJPKFNFCWJBCX-UHFFFAOYSA-N

Biochem./physiol. Wirkung

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.

Piktogramme

Exclamation mark
GHS07

Signalwort

Warning

H-Sätze

H302

Gefahreneinstufungen

Acute Tox. 4 Oral

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

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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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