Cat. #151711
MGMT inhibitor Lomeguatrib Small Molecule (Tool Compound)
Cat. #: 151711
Sub-type: Inhibitor
Availability: Please enquire for quantities and pricing
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...
This fee is applicable only for non-profit organisations. If you are a for-profit organisation or a researcher working on commercially-sponsored academic research, you will need to contact our licensing team for a commercial use license.
Contributor
Inventor: Geoffrey Margison
Institute: Cancer Research UK, Manchester Institute
Tool Details
*FOR RESEARCH USE ONLY
- Tool name: MGMT inhibitor Lomeguatrib Small Molecule (Tool Compound)
- Alternate name: PaTrin 2
- Molecular formula: C10H8BrN5OS
- Tool sub type: Inhibitor
- Primary target: DNA repair protein MGMT and related mammalian proteins
- 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.
- 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
- Iupac: 2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine
- Molecular weight: 326.17
Handling
- Purity: 326.17 g/mol
- Storage conditions: Ambient
- Shipping conditions: Dry Ice
Target Details
- Primary target: DNA repair protein MGMT and related mammalian proteins
- Ic50: 5 nM
Application Details
- 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...
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)
