Inactivator of O6-methylguanine-DNA methyltransferase
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Lomeguatrib

Item No. 11732

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[(4-bromo-2-thienyl)methoxy]-9H-purin-2-amine
CAS Number
192441-08-0
Synonyms
  • PaTrin 2
Molecular Formula
C10H8BrN5OS
Formula Weight
326.2
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 5 mg/ml
λmax
239, 284 nm
SMILES
BrC1=CSC(COC2=NC(N)=NC3=C2NC=N3)=C1
InChi Code
InChI=1S/C10H8BrN5OS/c11-5-1-6(18-3-5)2-17-9-7-8(14-4-13-7)15-10(12)16-9/h1,3-4H,2H2,(H3,12,13,14,15,16)
InChi Key
JUJPKFNFCWJBCX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $42

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    10 mg

    $74

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    25 mg

    $161

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    50 mg

    $303

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    Cayman Chemical
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    Product Description

    Lomeguatrib is a modified quanine base which acts as a pseudosubstrate inactivator of MGMT (IC50 = ~3 nM).1,2 A non-toxic compound, lomeguatrib completely inactivates MGMT in human prostate and colorectal tumors when given as a single 120 mg oral dose and in primary central nervous system cancers at 160 mg.3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Clemons, M., Kelly, J., Watson, A.J., et al. O6-(4-bromothenyl)guanine reverses temozolomide resistance in human breast tumour MCF-7 cells and xenografts. Br. J. Cancer 93(10), 1152-1156 (2005).

    2. McMurry, T.B.H. MGMT inhibitors-the Trinity College-Paterson Institute experience, a chemist’s perception. DNA Repair 6(8), 1161-1169 (2007).

    3. Ranson, M., Middleton, M.R., Bridgewater, J., et al. Lomeguatrib, a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase: Phase I safety, pharmacodynamic, and pharmacokinetic trial and evaluation in combination with temozolomide in patients with advanced solid tumors. Clin. Cancer Res. 12(5), 1577-1584 (2006).

    4. Watson, A.J., Sabharwal, A., Thorncroft, M., et al. Tumor O6-methylguanine-DNA methyltransferase inactivation by oral lomeguatrib. Clin. Cancer Res. 16(2), 743-749 (2010).