Lomeguatrib

SKU: orb1223211

Description

Lomeguatrib, also known as PaTrin-2, is a potent Inhibitor of O6-Alkylguanine-DNA-Alkyltransferase. Lomeguatrib is also a nontoxic low-molecular weight pseudosubstrate that has the ability to inactivate MGMT. Lomeguatrib can be used with temozolomide (TMZ) for GBM treatment.(In Vitro):Lomeguatrib (Compound 10) is a O6-methylguanine methyltransferase (MGMT) inhibitor, with an IC50 of 9 nM in cell-free assay and ～6 nM in MCF-7 cells. Lomeguatrib (10 μM) substantially increases the growth inhibitory effects of temozolomide in MCF-7 cells (D60=10 μM with Lomeguatrib vs 400 μM without).(In Vivo):Lomeguatrib (20 mg/kg i.p.) completely inactivates MGMT within 2 h, but shows no significant effect on tumor growth in MCF-7 xenografts.

Key Properties

• CAS Number: 192441-08-0
• MW: 326.17
• Purity: >98% (HPLC)
• Formula: C₁₀H₈BrN₅OS
• SMILES: Nc1nc2c([nH]cn2)c(OCc2cc(Br)cs2)n1
• Target: Antifungal
• Solubility: DMSO : ≥ 56 mg/mL; 171.69 mM

Bioactivity

• In Vivo:
  Lomeguatrib (20 mg/kg i.p.) completely inactivates MGMT within 2 h, but shows no significant effect on tumor growth in MCF-7 xenografts.
• In Vitro:
  Lomeguatrib (Compound 10) is a O6-methylguanine methyltransferase (MGMT) inhibitor, with an IC50 of 9 nM in cell-free assay and ~6 nM in MCF-7 cells. Lomeguatrib (10 μM) substantially increases the growth inhibitory effects of temozolomide in MCF-7 cells (D60=10 μM with Lomeguatrib vs 400 μM without).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PaTrin 2 | PaTrin2 | PaTrin-2 | Lomeguatrib

Quick Database Links

Gene Symbol

Antifungal