Lomeguatrib

Cat. No. 4359

Lomeguatrib C10H8BrN5OS [192441-08-0]

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Alternative Name: PaTrin-2

Chemical Name: 6-[(4-Bromo-2-thienyl)methoxy]-9H-purin-2-amine

Biological Activity

Inhibitor of O6-methylguanine-DNA methyltransferase (MGMT); (IC50 = 0.009 μM in cell-free extracts from HeLa S3 cells); attenuates MGMT activity in vitro and in vivo. Enhances the antitumor activity of temozolomide (Cat. No. 2706) in both human melanoma and MCF-7 xenografts.

Technical Data

M.Wt:
326.17
Formula:
C10H8BrN5OS
Solubility:
Soluble to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
192441-08-0

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Clemons et al (2005) O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumor MCF-7 cells and xenografts. Br.J.Cancer 93 1152. PMID: 16278661.

Barvaux et al (2004) Sensitization of a human ovarian cancer cell line to temozolomide by simultaneous attenuation of the Bcl-2 antiapoptotic protein and DNA repair by O6-alkylguanine-DNA alkyltransferase. Mol.Cancer Ther. 3 1215. PMID: 15486188.

Reinhard et al (2001) Monosaccharide-linked inhibitors of O6-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships. J.Med.Chem. 44 4050. PMID: 11708909.

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Keywords: Lomeguatrib, supplier, dna, mgmt, o6-methylguanine-dna, methyltransferases, inhibitors, inhibits, psuedosubstrates, epigenetics, Tocris Bioscience, DNA Methyltransferase Inhibitor products

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