#151711

MGMT inhibitor Lomeguatrib Small Molecule (Tool Compound)

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Cat. #151711

MGMT inhibitor Lomeguatrib Small Molecule (Tool Compound)

Cat. #: 151711

Sub-type: Inhibitor

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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...

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Contributor

Inventor: Geoffrey Margison

Institute: Cancer Research UK, Manchester Institute

Tool Details
Handling
Target Details
Application Details
References

Tool Details

*FOR RESEARCH USE ONLY

  • Tool name: MGMT inhibitor Lomeguatrib Small Molecule (Tool Compound)
  • Alternate name: PaTrin 2
  • Research fields: Cell signaling and signal transduction
  • 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)