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Lomeguatrib

Cat. No. 4359

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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.

Resources

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch

Safety Data Sheet: View Safety Data Sheet

References

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.

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.

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.

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