DC Chemicals · Product datasheet

Lomeguatrib(PaTrin-2) — Datasheet

CAT. NO. DC7188

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ParameterValue
Chemical NameLomeguatrib
CAS No.192441-08-0
SynonymsLomeguatrib;2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine;2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine O6-(4-bromothenyl)guanine;6-[(4-bromothiophen-2-yl)methoxy]-7H-purin-2-amine;PaTrin 2;PaTrin-2;O6-(4-bromothenyl)guanine;C521206;Lomeguqtrib;Lomeguaritrib;LoMeguatrib(PaTrin-2);6-((4-Bromo-2-thienyl)methoxy)purin-2-amine;6-[(4-BroMo-2-thienyl)Methoxy]-9H-purin-2-aMine;6-[(4-BroMo-2-thienyl)Methoxy] -1H-purin-2-aMine;Lomeguatrib, >=98%;6-(4-Bromothenyloxy)-7H-purin-2-amine;S79265T71M;6-((4-Bromo-2-thienyl)methoxyl)purin-2-amine;6-((4-bromothiophen-2-yl)methoxy)-7H-purin-2-amine;1H-Purin-2-amine, 6-[(4-bromo-2-thienyl)methoxy]-;Lomeguatrib [INN];Lomeguatrib [INN:BAN];O(6)-(4-bromothenyl)guanine;6-((4-brom
FormulaC10H8BrN5OS
M.Wt326.1724
SMILESBrC1=C([H])SC(=C1[H])C([H])([H])OC1C2=C(N=C(N([H])[H])N=1)N=C([H])N2[H]
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

Lomeguatrib is a O6-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC50s of 9 nM in cell-free assay and ∼6 nM in MCF-7 cells.

In Vitro

Lomeguatrib (Compound 10) is a O6-methylguanine methyltransferase (MGMT) inhibitor, with an IC50 of 9 nM in cell-free assay[1] 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)[2].

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[2].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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