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Lomeguatrib

CAS No. 192441-08-0

Lomeguatrib( PaTrin 2 | PaTrin2 | PaTrin-2 | Lomeguatrib )

Catalog No. M17403 CAS No. 192441-08-0

Lomeguatrib, a modified guanine base, inhibits the activity of DNA repair protein O(6)-alkylguanine-DNA alkyltransferase (MGMT) .

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 46 In Stock
5MG 41 In Stock
10MG 51 In Stock
25MG 90 In Stock
50MG 151 In Stock
100MG 276 In Stock
200MG Get Quote In Stock
500MG 691 In Stock
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Biological Information

  • Product Name
    Lomeguatrib
  • Note
    Research use only, not for human use.
  • Brief Description
    Lomeguatrib, a modified guanine base, inhibits the activity of DNA repair protein O(6)-alkylguanine-DNA alkyltransferase (MGMT) .
  • 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.
  • 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.
  • Synonyms
    PaTrin 2 | PaTrin2 | PaTrin-2 | Lomeguatrib
  • Pathway
    Microbiology/Virology
  • Target
    Antifungal
  • Recptor
    O6-alkylguanine-DNA-alkyltransferas
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    192441-08-0
  • Formula Weight
    326.17
  • Molecular Formula
    C10H8BrN5OS
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : ≥ 56 mg/mL; 171.69 mM
  • SMILES
    Nc1nc2c([nH]cn2)c(OCc2cc(Br)cs2)n1
  • Chemical Name
    2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. McElhinney RS, et al. J Med Chem, 1998, 41(26), 5265-5271.
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