Lomeguatrib

Catalog No.S8056 Synonyms: PaTrin-2

Lomeguatrib Chemical Structure

Molecular Weight(MW): 326.17

Lomeguatrib is a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase with IC50 of 5 nM.

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Cited by 2 Publications

2 Customer Reviews

  • Characterization of melanoma cell lines upon MGMT status. A, representative examples of dose-response curves for MGMT+ and MGMT− cells treated with temozolomide (TMZ) with or without lomeguatrib (LOM). Graphs show the average GI50 for temozolomide in the presence or absence of lomeguatrib (B).

    Mol Cancer Ther, 2015, 14(5):1236-46.. Lomeguatrib purchased from Selleck.

    T98G cells were pretreated with Lom (10 µM) for 1 hour, following the addition of TMZ (250 µM) over 48 hours. Protein levels of MGMT were detected via immunoblotting.

    Onco Targets Ther, 2018, 11:3671-3684. Lomeguatrib purchased from Selleck.

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Biological Activity

Description Lomeguatrib is a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase with IC50 of 5 nM.
Targets
O6-alkylguanine-DNA-alkyltransferas [1]
()
5 nM
In vitro

Lomeguatrib inactivates O6-alkylguanine-DNA-alkyltransferase (ATase) with a IC50 10-fold lower than O6-Benzylguanine. Lomeguatrib inhibits the activity of ATase in Raji cells with IC50 of 10 nM. [1] Lomeguatrib effectively inactivates MGMT in MCF-7 cells with IC50 of ~6nM ). 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/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. [2] 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 complete ATase depletion in tumor within 2 hr. Temozolomide (100 g/kg/day) significantly delays growth of the A375M tumour xenograft with an estimated delay in the time for tumour to quintuple in size of 9.6 days. Addition of Lomeguatrib to temozolomide significantly enhances the latter’s effect, delaying the quintupling time a further 8.7 days. Moreover, the Lomeguatrib combination results in considerably less toxicity (0/9 vs. 2/9 deaths; 6.84% weight loss vs. 9.48%). Lomeguatrib alone has no significant effect on tumour growth. [3]

Protocol

Solubility (25°C)

In vitro DMSO 65 mg/mL (199.28 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 326.17
Formula

C10H8BrN5OS

CAS No. 192441-08-0
Storage powder
in solvent
Synonyms PaTrin-2

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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID