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MGMT inhibitor Lomeguatrib Small Molecule (Tool Compound)

Info

Catalogue Number 151711
Antigen/Gene or Protein Targets DNA repair protein MGMT and related mammalian proteins
Synonyms PaTrin 2
Type Inhibitor
Relevance 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.
On Target IC50 5 nM
Molecular Formula C10H8BrN5OS
lUPAC 2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine
Molecular Weight (g/mol) 326.17
In vivo applications 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 complete ATase depletion in tumor within 2 hr. Moreover, the Lomeguatrib combination results in considerably less toxicity (0/9 vs. 2/9 deaths; 6.84% weight loss vs. 9.48%). Lomeguatrib alone has no significant effect on tumour growth.
In vitro applications Lomeguatrib inactivates O6-alkylguanine-DNA-alkyltransferase (ATase) with a IC50 10-fold lower than O6-Benzylguanine. Lomeguatrib inhibits the activity of ATase in Raji cells with IC50 of 10 nM. Lomeguatrib effectively inactivates MGMT in MCF-7 cells with IC50 of ~6nM. Lomeguatrib (10 μM ) substantially increases the growth inhibitory effects of temozolomide in MCF-7 cells (D60= 10 μM with Lomeguatrib vs 400 μM without).
Research Area DNA Damage and Repair, Epigenetics & Nuclear Signalling
Storage Ambient

References: 4 entries

Watson et al. 2010. Clin Cancer Res. 16(2):743-9. PMID: 20068091.

Khan et al. 2008. Br J Cancer. 98(10):1614-8. PMID: 18475294.

Ranson et al. 2006. Clin Cancer Res. 12(5):1577-84. PMID: 16533784.

Clemons et al. 2005. Br J Cancer. 93(10):1152-6. PMID: 16278661.


Add a reference

References: 4 entries

Watson et al. 2010. Clin Cancer Res. 16(2):743-9. PMID: 20068091.

Khan et al. 2008. Br J Cancer. 98(10):1614-8. PMID: 18475294.

Ranson et al. 2006. Clin Cancer Res. 12(5):1577-84. PMID: 16533784.

Clemons et al. 2005. Br J Cancer. 93(10):1152-6. PMID: 16278661.


Add a reference

References: 4 entries

Watson et al. 2010. Clin Cancer Res. 16(2):743-9. PMID: 20068091.

Khan et al. 2008. Br J Cancer. 98(10):1614-8. PMID: 18475294.

Ranson et al. 2006. Clin Cancer Res. 12(5):1577-84. PMID: 16533784.

Clemons et al. 2005. Br J Cancer. 93(10):1152-6. PMID: 16278661.


Add a reference


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