MGMT inhibitor Lomeguatrib Small Molecule (Tool Compound)

The MGMT inhibitor Lomeguatrib is a potent inhibitor of O6-alklguanine-DNA-alkyltransferase. It shows antitumoral activity in vivo in combination with the compound Temozolomide.

Contributors

Inventor Institute
Geoffrey Margison Cancer Research UK, Manchester Institute
Cat. #: 151711
Tool sub type: Inhibitor
Research Fields: Cell signaling and signal transduction
Application: Lomeguatrib (20 mg/kg/day for 5 days) combined with Temozolomide (100 mg/kg/day for 5 days) produces a substantial tumour growth delay: median tumour quintupling time is increased by 22 days without any significant increase in toxicity, while neither of the two drugs administrated along show any antitumor activity. Lomeguatrib inactivates ATase and enhances the anti-tumour effect of Temozolomide in A375M human melanoma xenografts model. Lomeguatrib, at a single dose of 20 mg/kg i.p., produces…
Purpose: Inhibitor
Alternate name: PaTrin 2
Product description: The MGMT inhibitor Lomeguatrib is a potent inhibitor of O6-alklguanine-DNA-alkyltransferase. It shows antitumoral activity in vivo in combination with the compound Temozolomide.
Molecular weight: 326.17
Primary target: DNA repair protein MGMT and related mammalian proteins
Storage conditions: Ambient
Shipping conditions: Dry Ice
References:

Barvaux et al. 2004. Mol Cancer Ther. 3: 1215-20 (PMID: 15426188) Clemons et al. 2005. Br J Cancer. 93: 1152-6 (PMID: 16278661) Ranson et al. 2006. Clin Cancer Res. 12: 1577-84 (PMID: 16533784) Khan et al. 2008 Br J Cancer. 98: 1614-8 (PMID: 18475294) Watson et al. 2010. Clin Cancer Res. 16: 743-9 (20068091)

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